| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| AGI 6780 | Axon 2274
CAS [1432660-47-3]
MF C21H18F3N3O3S2MW 481.51
Purity:
99%
Soluble in DMSO
Description
Inhibitor of isocitrate dehydrogenases (IDH) selective for mutant IDH2.
AGI 6780 potently and selectively inhibits the tumor-associated mutant IDH2/R140Q (EC50 value <20 nM for reduction of 2HG levels in cell lines) in an allosteric manner at the dimer interface, and induces differentiation of TF-1 erythroleukemia and primary human acute myelogenous leukemia cells in vitro.
References
Certificates
Categories
Extra info
F. Wang et al. Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation. Science. 2013, 340, 622-626.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Epigenetics
EC 1.1.1.42
Stem Cell Differentiator
IDH
Potent and selective inhibitor of the tumor-associated mutant IDH2 (R140Q)
Chemical name
N-cyclopropyl-4-(thiophen-3-yl)-3-(3-(3-(trifluoromethyl)phenyl)ureido)benzenesulfonamide
Parent CAS No.
[1432660-47-3]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| AGI 5198 - IDH-C35 | Axon 2122
CAS [1355326-35-0]
MF C27H31FN4O2MW 462.56
Purity:
100%
Soluble in DMSO
Description
Potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1); selective for IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 and 0.16 µM, respectively; it delays growth and promotes differentiation of glioma cells.
KEYWORDS: AGI 5198 | supplier | IDH1 inhibitor | IDH-C35 | CAS [1355326-35-0] | Isocitrate | IDH | Inhibitor | Enzymes | | axonmedchem |
| EBPC | Axon 1204
CAS [4450-98-0]
MF C14H15NO4MW 261.27
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent aldose reductase inhibitor
References
Certificates
Categories
Extra info
EK Lee et al. Inhibition of aldose reductase enhances HeLa cell sensitivity to chemotherapeutic drugs and involves activation of extracellular signal-regulated kinases. Anti-Cancer Drugs. 2002, 13(8), 859-868.
BL Mylari et al. A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate and its congeners. J. Med. Chem. 1991, 34, 1011.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Aldose reductase
EC 1.1.1.21
Aldose reductase inhibitor
Chemical name
1-Benzyl-4-hydroxy-5-oxo-2,5-dihydro-1H-pyrrole-3-carboxylic acid ethyl ester
Parent CAS No.
[4450-98-0]
Order
Size
Unit Price
Stock
10 mg
€82.00
In Stock | | axonmedchem |
| BVT 2733 hydrochloride | Axon 1756
CAS [376641-65-5]
MF C17H21ClN4O3S2.HClMW 465.42
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1
References
Certificates
Categories
Extra info
P Alberts et al. Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains. Endocrinology. 2003, 144(11), 4755-4762.
SJ Wang et al. Inhibition of 11beta-hydroxysteroid dehydrogenase type 1 reduces food intake and weight gain but maintains energy expenditure in diet-induced obese mice. Diabetologia. 2006, 49(6), 1333-7.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Dehydrogenase (11β-hydroxysteroid, type 1)
EC 1.1.1.146
Inhibitor of 11β-hydroxysteroid dehydrogenase type 1
Chemical name
3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide hydrochloride
Parent CAS No.
[376640-41-4]
Order
Size
Unit Price
Stock
5 mg
€115.00
In Stock | | axonmedchem |
| 6,8-Bis(benzylthio)octanoic acid | Axon 2125
CAS [95809-78-2]
MF C22H28O2S2MW 388.59
Purity:
100%
Soluble in 0.1N NaOH(aq) and DMSO
Description
A small molecular inhibitor of a mitochondrial enzyme pyruvate dehydrogenase (PDH) complex; 6,8-bis(benzylthio)octanoic acid selectively attacks the regulatory aspects of tumor cell mitochondrial metabolism, activating both apoptotic (programmed cell death) and non-apoptotic (necrosis-like) cell death pathways.
KEYWORDS: 6,8-Bis(benzylthio)octanoic acid | PDH inhibitor | CAS [95809-78-2] | Pyruvate | PDH | Inhibitor | Enzymes | | axonmedchem |
| AG-120 - Ivosidenib | Axon 2746
CAS [1448347-49-6]
MF C28H22ClF3N6O3MW 582.96
Purity:
99%
Optical purity:
99.9% e.e.
Soluble in DMSO
Description
AG-120 (Ivosidenib) is an oral, selective, first-in-class, potent inhibitor of mutant IDH1. Treatment with AG-120 decreased intracellular 2-HG levels, inhibited growth factor independent proliferation and restored erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells. Similarly, pharmacological inhibition of mutant IDH1 enzyme with AG-120 in primary human blast cells cultured ex vivo provided an effective way to lower intracellular 2-HG levels and induced myeloid differentiation.
KEYWORDS: AG-120 | supplier | IDH1 inhibitor | Ivosidenib | AG120 | AG 120 | CAS [1448347-49-6] | Isocitrate | IDH | Inhibitor | Enzymes | | axonmedchem |
| ASP 9521 | Axon 2787
CAS [1126084-37-4]
MF C19H26N2O3MW 330.42
Purity:
99%
Soluble in DMSO
Description
ASP 9521 is a novel, selective, orally bioavailable inhibitor of 17β–hydroxysteroid dehydrogenase type 5 (17β-HSD5; AKR1C3) with IC50 values of 11 and 49 nM in recombinant human and cynomolgus monkey AKR1C3, respectively.
KEYWORDS: ASP 9521 | supplier | 17β-HSD5 inhibitor | ASP9521 | ASP-9521 | CAS [1126084-37-4] | Dehydroepiandrosterone | Androstenedione | Dehydrogenase (17β-hydroxysteroid | type 5) | Inhibitor | Enzymes | AKR1C3 | Prostate cancer | | axonmedchem |
| AG-221 - Enasidenib | Axon 2745
CAS [1446502-11-9]
MF C19H17F6N7OMW 473.37
Purity:
99%
Soluble in DMSO
Description
AG-221 (Enasidenib) is an oral, selective, first-in-class inhibitor of the mutant IDH2 enzyme (IC50 value of 100 nM). AG-221 demonstrates excellent pharmaceutical properties, including adequate solubility, low clearance, and good oral bioavailability, and potently inhibits 2HG production by both the IDH2R140Q/WT heterodimer and IDH2R140Q homodimer. AG-221 suppressed 2HG production and induced cellular differentiation in primary human IDH2 mutation–positive acute myeloid leukaemia (AML) cells ex vivo and in xenograft mouse models.
KEYWORDS: AG-221 | supplier | IDH2 inhibitor | Enasidenib | AG 221 | AG221 | CAS [1446502-11-9] | Isocitrate | IDH | Inhibitor | Enzymes | | axonmedchem |
| APPA | Axon 2883
CAS [100750-39-8]
MF C14H13NO3MW 243.26
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| Alda 1 | Axon 2551
CAS [349438-38-6]
MF C15H11Cl2NO3MW 324.16
Purity:
99%
Soluble in DMSO
Description
Small molecule activator of ALDH2 (EC50 value ca 6 μM for ALDH2 mediated acetaldehyde metabolism) with the ability to activate wild-type ALDH2 and restore near-wild-type activity to ALDH2*2. When administered to rats before an ischemic event, Alda 1 reduced infarct size by 60%, most likely through its inhibitory effect on the formation of cytotoxic aldehydes. Alda-1 was effective in protecting against rotenone-induced apoptotic cell death in both SH-SY5Y cells and primary cultured substantia nigra (SN) dopaminergic neurons, and significantly reduced rotenone- or MPTP-induced death of SN tyrosine hydroxylase (TH)-positive dopaminergic neurons.
KEYWORDS: Alda 1 | supplier | ALDH2 activator | Alda1 | CAS [349438-38-6] | Alcohol | ALDH | Activator | agonist | ALDH2*2 | dehydrogenase | alcoholism | ischemia | chaperone | neuroprotective | dopamine neurons | rotenone | MPTP | substantia nigra | | axonmedchem |
| DEAB - NSC 8782 | Axon 2476
CAS [120-21-8]
MF C11H15NOMW 177.24
Purity:
99%
Soluble in DMSO
Description
Potent inhibitor of cytosolic (class 1) aldehyde dehydrogenase (ALDH) enzymes (IC50 values 0.057 µM, 1.2 µM, 3.0 µM, 1.2 µM, 0.16 µM, and 13 µM for inhibition of ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, ALDH2, and ALDH5A1, respectively). DEAB was also found to be an excellent substrate for ALDH3A1, and an irreversible inhibitor of ALDH7A1 (KI value 100 µM). Low turn-over rates and/or covalent bonding of the ALDH substrate DEAB are the cause of its inhibitory effect on the enzymes. At the time of development DEAB was found to be a potent inhibitor of cytosolic ALDH1 but not mitochondrial ALDH2. Commonly used as “selective” inhibitor of ALDH isoenzymes in cancer stem cell biology.
References
Certificates
Categories
Extra info
C.A. Morgan et al. N,N-diethylaminobenzaldehyde (DEAB) as a substrate and mechanism-based inhibitor for human ALDH isoenzymes. Chem Biol Interact. 2015 Jun 5;234:18-28.
M.I.Mahmoud et al. Effect of 4-(diethylamino)benzaldehyde on ethanol metabolism in mice. Alcohol Clin Exp Res. 1993 Dec;17(6):1223-7.
M. Luo et al. Diethylaminobenzaldehyde is a covalent, irreversible inactivator of ALDH7A1. ACS Chem Biol. 2015 Mar 20;10(3):693-7.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Stem Cell
ALDH
EC 1.2.1.36
Potent inhibitor of cytosolic (class 1) aldehyde dehydrogenase (ALDH) enzymes
Chemical name
4-(diethylamino)benzaldehyde
Parent CAS No.
[120-21-8]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| RO 28-1675 - RO 28-0450, (R)- | Axon 1356
CAS [300353-13-3]
MF C18H22N2O3S2MW 378.51
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Description
Glucokinase GK activator; more active R-enantiomer of RO-28-0450 (Axon 1134) in comparison with S-enantiomer, RO 28-1674 (Axon 1355)
References
Certificates
Categories
Extra info
J Grimsby et al. Allosteric Activators of Glucokinase: Potential Role in Diabetes Therapy. Science Signaling 2003, 301(5631), 370-373.
T Kietzmann and GK Ganjam. Glucokinase: old enzyme, new target. Exp. Opin. Ther. Patents. 2005, 15(6), 705-713.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Glucokinase
EC 2.7.1.2
Glucokinase (GK) activator
Chemical name
(R)-(-)-3-Cyclopentyl-2-(4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide
Parent CAS No.
[300353-13-3]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| RO 28-1674 - RO 28-0450, (S)- | Axon 1355
CAS [599164-57-5]
MF C18H22N2O3S2MW 378.51
Purity:
99%
Optical purity:
99% ee
Soluble in DMSO
Description
Glucokinase GK activator; less active S-enantiomer of RO-28-0450 (Axon 1134), in comparison with R-enantiomer, RO 28-1675 (Axon 1356)
References
Certificates
Categories
Extra info
J Grimsby et al. Allosteric Activators of Glucokinase: Potential Role in Diabetes Therapy. Science Signaling 2003, 301(5631), 370-373.
T Kietzmann & GK Ganjam. Glucokinase: old enzyme, new target. Exp. Opin. Ther. Patents. 2005, 15(6), 705-713.
Certificate of Analysis
Material Safety Data Sheet
Diabetes & Metabolism
Glucokinase
EC 2.7.1.2
Glucokinase (GK) activator
Chemical name
(S)-(+)-3-Cyclopentyl-2-(4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide
Parent CAS No.
[599164-57-5]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| RO 28-0450 - RO 28-1675, (±)- | Axon 1134
CAS [300352-96-9]
MF C18H22N2O3S2MW 378.51
Purity:
98%
Soluble in DMSO
Description
Glucokinase GK activator; its more active (R)-enantiomer is RO-28-1675 (Axon 1356)
References
Certificates
Categories
Extra info
Grimsby et al. Allosteric Activators of Glucokinase: Potential Role in Diabetes Therapy. Science Signaling 18 July 2003: 370.
T Kietzmann and GK Ganjam. Glucokinase: old enzyme, new target. Exp. Opin. Ther. Pat. 2005, 15, 705-713.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
Glucokinase
EC 2.7.1.2
Glucokinase (GK) activator
Chemical name
3-Cyclopentyl-2-(4-methanesulfonyl-phenyl)-N-thiazol-2-yl-propionamide
Parent CAS No.
[300352-96-9]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| Iniparib - BSI 201 | Axon 1566
CAS [160003-66-7]
MF C7H5IN2O3MW 292.03
Purity:
99%
Soluble in DMSO
Description
An irreversible inhibitor of poly(ADP-ribose) polymerase-1 (PARP 1); it inhibits PARP1, a nuclear enzyme that promotes DNA repair through the base-excision repair pathway; potential therapeutic undergoing clinical trials for treatment of some types of breast cancer
References
Certificates
Categories
Extra info
A Patel and SH Kaufmann. Development of PARP Inhibitors: An Unfinished Story. ONCOLOGY. 2010, Vol. 24 No. 1.
J O'Shaughnessy et al. Iniparib plus Chemotherapy in Metastatic Triple-Negative Breast Cancer. N. Engl. J. Med. 2011, 364, 205-214.
LA Carey and NE Sharpless. PARP and Cancer — If It's Broke, Don't Fix It. N. Engl. J. Med. 2011, 364, 277-279.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 2.4.2.30
PARP
PARP inhibitor
Chemical name
4-iodo-3-nitrobenzamide
Parent CAS No.
[160003-66-7]
Order
Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Aminobenzamide, 3- - AB, 3- | ABA, 3- | Axon 1496
CAS [3544-24-9]
MF C7H8N2OMW 136.15
Purity:
99%
Soluble in water and DMSO
Description
A competitive small molecule inhibitor of poly(ADP-ribose) polymerase (PARP)
References
Certificates
Categories
Extra info
S Cuzzocrea et al. Beneficial effects of 3‐aminobenzamide, an inhibitor of poly (ADP‐ribose) synthetase in a rat model of splanchnic artery occlusion and reperfusion. Br. J. Pharmacol. 1997, 121(6), 1065-1074.
MR Purnell and WJ Whish. Novel inhibitors of poly (ADP-ribose) synthetase. Biochem. J. 1980, 185(3), 775.
B Zingarelli et al. Protection against myocardial ischemia and reperfusion injury by 3-aminobenzamide, an inhibitor of poly (ADP-ribose) synthetase. Cardiovas. Res. 1997, 36(2), 205-215.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 2.4.2.30
PARP
Competitive small molecule inhibitor of PARP
Chemical name
3-aminobenzamide
Parent CAS No.
[3544-24-9]
Order
Size
Unit Price
Stock
10 mg
€45.00
In Stock | | axonmedchem |
| Sitamaquine - WR 6026 tosylate | Axon 1515
CAS [1019640-33-5]
MF C21H33N3O.C7H8O3SMW 515.71
Purity:
99%
Soluble in DMSO
Description
Dose-dependent and orally available inhibitior of complex II (succinate dehydrogenase or SDH) of the respiratory chain in digitonin-permeabilized promastigotes. A potential agent as an oral treatment of life-threatening visceral leishmaniasis (VL) caused by Leishmania donovani (EC50 value 19.8 μM for L. donovani promastigotes in vitro).
References
Certificates
Categories
Extra info
A.M. Dueñas-Romero et al. Interaction of sitamaquine with membrane lipids of Leishmania donovani promastigotes. Biochim. Biophys. Acta. 2007, 1768, 246-252.
C. López-Martín et al. Sitamaquine sensitivity in Leishmania species is not mediated by drug accumulation in acidocalcisomes. Antimicrob. Agents Chemother. 2008, 52, 4030-4036.
L. Carvalho et al. The 8-aminoquinoline analogue sitamaquine causes oxidative stress in Leishmania donovani promastigotes by targeting succinate dehydrogenase. Antimicrob. Agents Chemother. 2011, 55, 4204-4210.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Diabetes & Metabolism
Immunology
Succinate dehydrogenase
EC 1.3.5.1
Succinate dehydrogenase inhibitor with anti-Leishmanial activity
Chemical name
N,N-Diethyl-N'-(6-methoxy-4-methyl-quinolin-8-yl)-hexane-1,6-diamine tosylate
Parent CAS No.
[57695-04-2]
Order
Size
Unit Price
Stock
10 mg
€120.00
In Stock | | axonmedchem |
| AZD 2281 - Olaparib | KU 0059436 | Axon 1464
CAS [763113-22-0]
MF C24H23FN4O3MW 434.46
Purity:
99%
Soluble in DMSO
Description
Highly potent, oral and selective inhibitor of poly(ADP-ribose) polymerase (PARP); with IC50 = 5nM (PARP-1) and 1 nM (PARP-2). It blocks enzymes that repair DNA damage caused by cancer treatments such as radiation and drugs.
KEYWORDS: AZD 2281 | supplier | PARP inhibitor | Olaparib | KU 0059436 | AZD2281 | KU0059436 | AZD-2281 | KU-0059436 | CAS [763113-22-0] | DNA-RNA | poly-(ADP-ribose) polymerase | PARP-1 | PARP-2 | DNA damage | double strand break | DSB | CHK | | axonmedchem |
| NU 1025 | Axon 1370
CAS [90417-38-2]
MF C9H8N2O2MW 176.17
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent inhibitor of poly(ADP-ribose) polymerase (PARP); reported to have neuroprotective effects
References
Certificates
Categories
Extra info
R Kaundal et al. Neuroprotective effects of NU1025, a PARP inhibitor in cerebral ischemia are mediated through reduction in NAD depletion and DNA fragmentation. Life Sciences 2006, 79(24), 2293-302.
KJ Bowman et al. Potentiation of anti-cancer agent cytotoxicity by the potent poly(ADP-ribose) polymerase inhibitors NU1025 and NU1064. Br. J. Cancer. 1998, 78 1269.
CA Delaney et al. Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines. Clin. Cancer Res. 2000, 6, 2860.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 2.4.2.30
PARP
PARP inhibitor
Chemical name
8-Hydroxy-2-methyl-3H-quinazolin-4-one
Parent CAS No.
[90417-38-2]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| DR 2313 | Axon 1268
CAS [284028-90-6]
MF C8H10N2OSMW 182.24
Purity:
99%
Soluble in water and DMSO
Description
Potent PARP inhibitor; with neuroprotective effects, potentially more useful in treating acute stroke than a free radical scavenger
References
Certificates
Categories
Extra info
H Nakajima et al. A Newly Synthesized Poly(ADP-Ribose) Polymerase Inhibitor, DR2313 [2-Methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]. J. Pharmacol. Exp. Ther. 2005, 312(2), 312, 472-481.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
DNA-damage Response
EC 2.4.2.30
PARP
PARP inhibitor
Chemical name
1,5,7,8-Tetrahydro-2-methyl-4H-thiopyrano[4,3-D]Pyrimidin-4-one
Parent CAS No.
[284028-90-6]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Niraparib - MK 4827 | Axon 2928
CAS [1038915-60-4]
MF C19H20N4OMW 320.39
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO
Description
Niraparib is a potent, selective and orally available PARP 1/2 inhibitor with IC50 values of 3.8 and 2.1 nM, respectively. Moreover, in a whole cell assay, Niraparib inhibited PARP activity with an EC50 value of 4 nM and inhibited proliferation of cancer cells with mutant BRCA-1 and BRCA-2 (CC50 value of 10−100 nM). Niraparib was well tolerated in vivo and demonstrated efficacy as a single agent in a xenograft model of BRCA-1 deficient cancer.
KEYWORDS: Niraparib | supplier | PARP inhibitor | MK 4827 | MK4827 | MK-4827 | CAS [1038915-60-4] | CAS [1038915-64-8] | CAS [1038915-73-9] | DNA-RNA | PARP | Inhibitor | Enzymes | BRCA | | axonmedchem |
| ABT 888 dihydrochloride - Veliparib dihydrochloride | A 861695 dihydrochloride | Axon 2888
CAS [912445-05-7]
MF C13H1N4O.2HClMW 317.21
Purity:
99%
Optical purity:
Optically pure
Soluble in water and DMSO
Description
Potent and orally bioavailable PARP inhibitor, with Ki values to be 5.2 nM for PARP1 and 2.9 nM for PARP2 respectively; inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents.
The free base of ABT 888 is available as Axon 1893.
KEYWORDS: ABT 888 dihydrochloride | supplier | PARP inhibitor | Veliparib dihydrochloride | A 861695 dihydrochloride | A861695 dihydrochloride | A-861695 dihydrochloride | CAS [912445-05-7] | [912444-00-9] | DNA-RNA | PARP | Inhibitor | Enzymes | | axonmedchem |
| ME0328 | Axon 2759
CAS [1445251-22-8]
MF C19H19N3O2MW 321.37
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
ME0328 is a potent, cell-permeable, selective inhibitor of PARP3/ARTD3 (IC50 value of 0.9 μM).
KEYWORDS: ME0328 | supplier | PARP inhibitor | ME 0328 | ME-0328 | CAS [1445251-22-8] | DNA-RNA | PARP | Inhibitor | Enzymes | ARTD3 | PARP3 | | axonmedchem |
| Piperlongumine - Piplartine | Axon 2488
CAS [20069-09-4]
MF C17H19NO5MW 317.34
Purity:
99%
Soluble in DMSO
Description
Natural alkaloid with potent cytotoxic activity which has been related to an increased reactive oxygen species (ROS) generation in cancer cells (through direct GSTP1 interaction), down-regulation of nuclear factor-kB (NF-kB) activation and induction of rapid depletion of the androgen receptor (AR) in prostate cancer cells. Moreover, Piperlongumine (or Piplartine) was found to induce apoptosis and autophagy through modulation of the PI3K/Akt/mTOR pathway in human lung cancer cells, and potently inhibited ligand-stimulated STAT3 nuclear translocation.
KEYWORDS: Piperlongumine | supplier | Apoptosis inducer/GSTP1 inhibitor | Piplartine | CAS [20069-09-4] | Glutathion (GSH) | GSTP | STAT3 | Inhibitor | ROS | reactive oxygen species | ubiquitin | UPS | proteasome | NF-kB | androgen receptor | apoptosis | autophagy | PI3K/Akt/mTOR | JNK | STAT3 | Natural alkaloid | | axonmedchem |
| TH 588 hydrochloride | Axon 2272
CAS [N.A.]
MF C13H12ClN4.HClMW 331.63
Purity:
99%
Soluble in DMSO
Description
First-in-class MTH1 inhibitor (IC50 value 5.0 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells. Similar to TH 287, TH 588 shows no relevant inhibitory effect for any of the other tested nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, nor for other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase and ITPA).Replacement of the methyl group by a cyclopropyl substituent in TH 588 (compared to TH 287, Axon 2271) improved metabolic stability both in vitro and in vivo, while maintaining MTH1 potency.
References
Certificates
Categories
Extra info
H. Gad et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature 2014, 508, 215-221.
Y. Nakabeppu et al. MTH1, an oxidized purine nucleoside triphosphatase, prevents the cytotoxicity and neurotoxicity of oxidized purine nucleotides. DNA Repair 2006, 5, 761-772.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
DNA-damage Response
MTH1
EC 3.6.1.56
First-in-class MTH1 inhibitor
Chemical name
N4-cyclopropyl-6-(2,3-dichlorophenyl)pyrimidine-2,4-diamine hydrochloride
Parent CAS No.
[1609960-31-7]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| PS 48 | Axon 1659
CAS [1180676-32-7]
MF C17H15ClO2MW 286.75
Purity:
99%
Soluble in DMSO and Ethanol
Description
Allosteric activator of phosphoinositide-dependent protein kinase 1 (PDPK1 or PDK1). PS 48 has a Z-configuration in comparison with its inactive E-isomer PS 47 (Axon 1664)
KEYWORDS: PS 48 | supplier | PDK1 activator | PS48 | CAS [1180676-32-7 ] | Phosphatidylinositol | PDPK1 | allosteric | activator | phosphoinositide-dependent protein kinase 1 | PS 47 | PS47 | | axonmedchem |
| BX 912 | Axon 1130
CAS [702674-56-4]
MF C20H23BrN8OMW 471.35
Purity:
99%
Soluble in 0.1N HCl(aq), DMSO, and Ethanol
Description
Inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDPK1).
KEYWORDS: BX 912 | supplier | PDK1 inhibitor | BX912 | BX-912 | CAS [702674-56-4] | Phosphatidylinositol | PDPK | Inhibitor | AGC | 3-Phosphoinositide-dependent Kinase-1 | PDPK-1 | PTEN | growth factor signaling | | axonmedchem |
| TH 287 hydrochloride | Axon 2271
CAS [N.A.]
MF C11H10Cl2N4.HClMW 305.59
Purity:
98%
Soluble in DMSO
Description
First-in-class MTH1 inhibitor (IC50 value 0.8 nM) that selectively and effectively kills U2OS and other cancer cell lines, with considerably less toxicity towards several primary or immortalized cells.
TH 287 shows no relevant inhibitory effect for any of the other tested nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, nor for other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase and ITPA).
References
Certificates
Categories
Extra info
H. Gad et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature 2014, 508, 215-221.
Y. Nakabeppu et al. MTH1, an oxidized purine nucleoside triphosphatase, prevents the cytotoxicity and neurotoxicity of oxidized purine nucleotides. DNA Repair 2006, 5, 761-772.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
DNA-damage Response
MTH1
EC 3.6.1.56
First-in-class MTH1 inhibitor
Chemical name
6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine hydrochloride
Parent CAS No.
[N.A.]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| ML 130 - Noditinib | Axon 1888
CAS [799264-47-4]
MF C14H13N3O2SMW 287.34
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of NOD1.
KEYWORDS: ML 130 | supplier | NOD1 inhibitor | Noditinib | ML130 | ML-130 | CAS [799264-47-4] | NF-κB Pathway | NOD1 | NLR | NACHT | leucine rich repeat domain containing proteins | innate | immunity | inflammation | apoptosis | | axonmedchem |
| Atglistatin | Axon 2276
CAS [1469924-27-3]
MF C17H21N3OMW 283.37
Purity:
98%
Soluble in DMSO
Description
Highly potent and selective inhibitor of adipose triglyceride lipase (ATGL; IC50 value 0.7 μM) that reduces fatty acid mobilization in vitro and in vitro.
Atglistatin does not inhibit HSL, monoglyceride lipase, pancreatic lipase, lipoprotein lipase and two lysophospholipases of the patatin-like phospholipase domain–containing protein family (PNPLA) exhibiting homology to ATGL.
References
Certificates
Categories
Extra info
N. Mayer et al. Development of small-molecule inhibitors targeting adipose triglyceride lipase. Nat. Chem. Biol. 2013, 9, 785-787.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Diabetes & Metabolism
ATGL
EC 3.1.1.3
Potent and selective inhibitor of adipose triglyceride lipase (ATGL)
Chemical name
3-(4'-(dimethylamino)biphenyl-3-yl)-1,1-dimethylurea
Parent CAS No.
[1469924-27-3]
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Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| CP 346086 | Axon 2216
CAS [186390-48-7]
MF C26H22F3N5OMW 477.48
Purity:
99%
Soluble in DMSO
Description
Potent microsomal triglyceride transfer protein (MTP, MTTP) inhibitor that inhibits both human and rodent MTP activity (IC50 value 2.0 nM). After a 2 week treatment CP 346086 reduced total and LDL cholesterol and triglycerides by 47%, 72%, and 75%, relative to either individual baselines or placebo, with little change in HDL cholesterol. More potent in MTP inhibition than SLX 4090 and Lomitapide (Juxtapid; IC50 value 8 nM and 5-7 nM respectively).
References
Certificates
Categories
Extra info
C.E. Chandler et al. CP-346086: an MTP inhibitor that lowers plasma cholesterol and triglycerides in experimental animals and in humans. J. Lipid. Res. 2003, 44, 1887-1901.
E. Kim et al. A small-molecule inhibitor of enterocytic microsomal triglyceride transfer protein, SLx-4090: biochemical, pharmacodynamic, pharmacokinetic, and safety profile. J. Pharmacol. Exp. Ther. 2011, 337, 775-785.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
MTP
Pfizer Licensed Products
Potent microsomal triglyceride transfer protein (MTP) inhibitor
Chemical name
N-(2-((1H-1,2,4-triazol-5-yl)methyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)-4'-(trifluoromethyl)biphenyl-2-carboxamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[186390-48-7]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| JZP 361 | Axon 2486
CAS [1680193-80-9]
MF C22H20ClN5OMW 405.88
Purity:
99%
Soluble in DMSO
Description
Selective reversible inhibitor of monoacylglycerol lipase (MAGL; IC50 value 46 nM) with 35-fold higher selectivity over human α/β-hydrolase-6 (ABHD6) and 150-fold higher selectivity over human FAAH. The Loratidine analog JZP 361 fully retained H1 antagonistic activity as well (pA2 value 6.81) but is devoid of cannabinoid receptor (CB) affinity.
KEYWORDS: JZP 361 | Supplier | MAGL inhibitor - H1 antagonist | JZP361 | CAS [1680193-80-9] | 2-arachidonoyl glycerol (2-AG) | MAGL | Inhibitor | antagonist | monoacylglycerol | lipase | histamine | allergy | Fatty acid amide hydrolase | FAAH | ABHD6 | | axonmedchem |
| Evacetrapib - LY 2484595 | Axon 2286
CAS [1186486-62-3]
MF C31H36F6N6O2MW 638.65
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, and selective inhibitor of cholesteryl ester transfer protein (CETP; IC 50 value 5.5 nM and 26 nM in human recombinant and plasme CETP assays, respectively) that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure.
References
Certificates
Categories
Extra info
G. Cao et al. Evacetrapib is a novel, potent, and selective inhibitor of cholesteryl ester transfer protein that elevates HDL cholesterol without inducing aldosterone or increasing blood pressure. J. Lipid Res. 2011, 52, 2169-2176.
D.G. Johns et al. On- and off-target pharmacology of torcetrapib: current understanding and implications for the structure activity relationships (SAR), discovery and development of CETP inhibitors. Drugs. 2012, 72, 491-507.
N.B. Mantlo et al. Update on the discovery and development of cholesteryl ester transfer protein inhibitors for reducing residual cardiovascular risk. J. Med. Chem. 2014, 57, 1-17.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Diabetes & Metabolism
CETP
Potent, and selective inhibitor of CETP
Chemical name
trans-(1S,4r)-4-(((S)-5-((3,5-bis(trifluoromethyl)benzyl)(2-methyl-2H-tetrazol-5-yl)amino)-7,9-dimethyl-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)methyl)cyclohexanecarboxylic acid
Parent CAS No.
[1186486-62-3]
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Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| Lomitapide - BMS 201038 | AEGR-733 | Axon 2917
CAS [182431-12-5]
MF C39H37F6N3O2MW 693.72
Purity:
98%
Soluble in DMSO
Description
Lomitapide is a highly potent microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 value of 0.5 nM. Moreover, lomitapide inhibited the production of lipoprotein particles in rodent models and normalized plasma lipoprotein levels in Watanabe-heritable hyperlipidemic (WHHL) rabbits, which are a model for human homozygous familial hypercholesterolemia.
KEYWORDS: Lomitapide | supplier | MTP inhibitor | BMS 201038 | AEGR-733 | BMS201038 | BMS-201038 | AEGR 733 | AEGR733 | CAS [182431-12-5] | CAS [202914-84-9] | CAS [182431-10-3] | Triglycerides | MTP | Inhibitor | Proteins | Hypercholesterolemia | | axonmedchem |
| URB602 | Axon 2696
CAS [565460-15-3]
MF C19H21NO2MW 295.38
Purity:
99%
Soluble in DMSO
Description
Non-competitive inhibitor of MAGL (monoacylglycerol lipase; IC50 values 25 μM and 17 μM for inhibition of hydrolysis of 2-oleoylglycerol (2-OG) and anandamide (AEA), respectively), lacking affinity for FAAH, diacylglycerol lipase or COX-2. URB602 blocks 2-AG hydrolysis in rat brain slices and enhances non-opioid stress-induced analgesia. Furthermore, URB602 reduced xenograft tumor volume, this effect being associated to down-regulation of VEGF and FGF-2, reduction in the number of vessels and down-regulation of cyclin D1.
KEYWORDS: URB602 | supplier | MAGL inhibitor | URB 602 | URB-602 | CAS [565460-15-3] | 2-arachidonoyl glycerol (2-AG) | MAGL | Inhibitor | Enzymes | | axonmedchem |
| MJN110 | Axon 2580
CAS [1438416-21-7]
MF C22H21Cl2N3O4MW 462.33
Purity:
98%
Soluble in DMSO
Description
Potent, selective, and in-vivo-active MAGL inhibitor (IC50 values 9.5 nM and 260 nM for inhibition of mouse MAGL and ABHD6, respectively) displaying strong antihyperalgesic activity (mechanical allodynia) in a rat model of diabetic neuropathy. MJN110 exhibits therapeutic potential in the treatment of acute nausea and vomiting as well as anticipatory nausea by elevation of endogenous cannabinoid 2-arachidonoylglycerol (2-AG) levels in the brain.
KEYWORDS: MJN110 | supplier | MAGL inhibitor | MJN-110 | CAS [1438416-21-7] | 2-arachidonoyl glycerol | 2-AG | MAGL | Inhibitor | endo-cannabinoid | ABHD6 | antihyperalgesic | allodynia | diabetic neuropathy | nausea | vomiting | | axonmedchem |
| A 922500 | Axon 2059
CAS [959122-11-3]
MF C26H24N2O4MW 428.48
Purity:
98%
Optical purity:
97% d.e.
Soluble in DMSO
Description
Highly potent and selective diacylglycerol acyltransferase (DGAT) isomer 1 (DGAT-1) inhibitor with nanomolar potency
References
Certificates
Categories
Extra info
G Zhao et al. Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J. Med. Chem. 2008, 51(3), 380-383.
AJ King et al. Diacylglycerol Acyltransferase 1 Inhibition Lowers Serum Triglycerides in the Zucker Fatty Rat and the Hyperlipidemic Hamster. J. Pharmacol. Exp. Ther. 2009, 330(2), 526-531.
AJ King et al. In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. Eur. J. Pharmacol. 2010, 637(1-3), 155-161.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
DGAT-1
EC 2.3.1.20
Highly potent and selective diacylglycerol acyltransferase 1 (DGAT-1) inhibitor
Chemical name
(1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)cyclopentanecarboxylic acid
Parent CAS No.
[959122-11-3]
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Size
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Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Torcetrapib - CP 529414 | Axon 2047
CAS [262352-17-0]
MF C26H25F9N2O4MW 600.47
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Cholesteryl ester transfer protein (CETP) inhibitor; a drug being developed to treat hypercholesterolemia (elevated cholesterol levels) and prevent cardiovascular disease
References
Certificates
Categories
Extra info
PJ Barter et al. Effects of torcetrapib in patients at high risk for coronary events. N. Engl. J. Med. 2007, 357(21), 2109-2122.
SE Nissen et al. Effect of Torcetrapib on the Progression of Coronary Atherosclerosis. N. Engl. J. Med. 2007, 356, 1304-1316.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Diabetes & Metabolism
CETP
Pfizer Licensed Products
Inhibitor of cholesterylester transfer protein (CETP)
Chemical name
(2R,4S)-ethyl 4-((3,5-bis(trifluoromethyl)benzyl)(methoxycarbonyl)amino)-2-ethyl-6-(trifluoromethyl)-3,4-dihydroquinoline-1(2H)-carboxylate
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[262352-17-0]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Atorvastatin calcium - Lipitor | Axon 2043
CAS [134523-03-8]
MF C33H34FN2O5.½CaMW 577.67
Purity:
99%
Soluble in DMSO
Description
An inhibitor of HMG-CoA reductase (statin) indicated as an adjunct therapy to diet to lower the LDL ("bad") cholesterol and triglycerides in your blood. It can raise your HDL ("good") cholesterol as well.
References
Certificates
Categories
Extra info
BD Roth. The Discovery and Development of Atorvastatin, a Potent Novel Hypolipidemic Agent. Prog. Med. Chem. 2002, 40, 1–22.
S Youssef et al. The HMG-CoA reductase inhibitor, atorvastatin, promotes a Th2 bias and reverses paralysis in central nervous system autoimmune disease. Nature 2002, 420, 78-84.
HM Colhoun et al. Primary prevention of cardiovascular disease with atorvastatin in type 2 diabetes in the Collaborative Atorvastatin Diabetes Study (CARDS): multicentre randomised placebo-controlled trial. Lancet, 2004, 364 (9435), 685 - 696.
PS Sever et al. Prevention of Coronary and Stroke Events with Atorvastatin in Hypertensive Patients who have Average or Lower-than-Average Cholesterol Concentrations, in the Anglo-Scandinavian Cardiac (...). Drugs 2004, 64 (2 Suppl.), 43-60.
JC LaRosa et al. Intensive Lipid Lowering with Atorvastatin in Patients with Stable Coronary Disease. N. Engl. J. Med. 2005, 352, 1425-1435.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
HMG-CoA reductase
EC 1.1.1.88
Pfizer Licensed Products
Inhibitor of HMG-CoA reductase
Chemical name
(3R,5R)-7-(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxyheptanoate hemi-calcium salt
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[134523-00-5]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| Dalcetrapib - JTT 705 | Axon 1962
CAS [211513-37-0]
MF C23H35NO2SMW 389.59
Purity:
99%
Soluble in DMSO and Ethanol
Description
Potent cholesterylester transfer protein (CETP) inhibitor
References
Certificates
Categories
Extra info
Z Huang et al. Cholesteryl ester transfer protein inhibitor (JTT-705) and the development of atherosclerosis in rabbits with severe hypercholesterolaemia. Clin Sci (Lond). 2002, 103(6), 587-594.
T.F. Lüscher et al. Vascular effects and safety of dalcetrapib in patients with or at risk of coronary heart disease: the dal-VESSEL randomized clinical trial. Eur. Heart J. 2012, 33(7), 857-865.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Diabetes & Metabolism
CETP
Unclassified
Inhibitor of cholesterylester transfer protein (CETP)
Chemical name
S-2-(1-(2-ethylbutyl)cyclohexanecarboxamido)phenyl 2-methylpropanethioate
Parent CAS No.
[211513-37-0]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| RUSKI-201 dihydrochloride | Axon 2673
CAS [N.A.]
MF C20H27N3OS.2HClMW 430.43
Purity:
98%
Optical purity:
Racemic
Soluble in water and DMSO
Description
Sonic Hedgehog acyltransferase (HHAT) inhibitor (IC50 value 0.20 μM) showing no off-target cytotoxicity, and quantitative whole-proteome palmitoylation profiling with a bioorthogonal alkyne-palmitate reporter. RUSKI-201 is the optimal tool molecule currently available to study HHAT function.
References
Certificates
Categories
Extra info
UR Rodgers et al. Characterization of Hedgehog Acyltransferase Inhibitors Identifies a Small Molecule Probe for Hedgehog Signaling by Cancer Cells. ACS Chem Biol. 2016 Dec 16;11(12):3256-3262.
X Zhang et al. Development of anticancer agents targeting the Hedgehog signaling. Cell Mol Life Sci. 2017 Mar 17.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
HHAT
Hedgehog
EC 2.3.1
Sonic HHAT inhibitor lacking off-target cytotoxicity
Chemical name
2-(2-methylbutylamino)-1-(4-(6-methylpyridin-2-yl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)ethanone dihydrochloride
Parent CAS No.
[1458031-48-5]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| IWP L6 | Axon 2212
CAS [1427782-89-5]
MF C25H20N4O2S2MW 472.58
Purity:
99%
Soluble in DMSO
Description
Highly potent porcupine inhibitor (Porcn; EC50 value 0.5 nM), a membrane-bound O-acyltransferase (MBOAT); Wnt signaling inhibitor; 60-times more potent than IWP-2.IWP-L6 effectively inhibits posterior axis formation and resected tailfin regeneration in juvenile zebrafish at low micromolar concentrations. IWP L6 specifically and reversibly blocks Wnt signaling and Wnt mediated branching morphogenesis in cultured mouse embryonic kidneys. Stable in human plasma over 24 h.
References
Certificates
Categories
Extra info
X. Wang et al. The development of highly potent inhibitors for porcupine. J. Med. Chem. 2013, 56, 2700-2704.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Porcupine
Wnt-β-Catenin
EC 2.3.1
Highly potent porcupine (Porcn) inhibitor
Chemical name
2-(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-ylthio)-N-(5-phenylpyridin-2-yl)acetamide
Parent CAS No.
[1427782-89-5]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| CP 775146 | Axon 2114
CAS [702680-17-9]
MF C26H33NO4MW 423.54
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective PPARα agonist (Ki=24.5 nM and >10 µM for PPARβ and PPARγ), supporting robust recruitment of co-activator peptides in vitro. CP775146 markedly potentiates chimeric transcription systems in cell-based assays and strikingly lowers serum triglycerides in vivo
References
Certificates
Categories
Extra info
CD Kane et al. Molecular characterization of novel and selective peroxisome proliferator-activated receptor alpha agonists with robust hypolipidemic activity in vivo. Mol. Pharmacol. 2009, 75(2), 296-306.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
PPAR
NR1C
Pfizer Licensed Products
Potent and selective PPARα agonist
Chemical name
(S)-2-(3-(1-(2-(4-isopropylphenyl)acetyl)piperidin-3-yl)phenoxy)-2-methylpropanoic acid
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[702680-17-9]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| RU-SKI 43 hydrochloride | Axon 2035
CAS [N.A.]
MF C22H30N2O2S.HClMW 423.01
Purity:
99%
Soluble in DMSO
Description
Hedgehog acyltransferase (HHAT) inhibitor in vitro and in cells; it blocks sonic hedgehog (Shh) signaling significantly
References
Certificates
Categories
Extra info
E Petrova et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling. Nature Chem. Biol. 2013, 9, 247–249.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
HHAT
Hedgehog
EC 2.3.1
Hedgehog acyltransferase (HHAT) inhibitor blocks Shh signaling
Chemical name
2-(2-methylbutylamino)-1-(4-(m-tolyloxymethyl)-6,7-dihydrothieno[3,2-c]pyridin-5(4H)-yl)ethanone hydrochloride
Parent CAS No.
[1043797-53-0]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| IWR-1-endo - IWR-1 | endo-IWR-1 | Axon 2510
CAS [1127442-82-3]
MF C25H19N3O3MW 409.44
Purity:
99%
Soluble in DMSO
Description
Small-molecule inhibitor of the Wnt/β-catenin pathway (IC50 value 0.18 μM), strongly inhibiting TNKS1 and TNKS2 in biochemical assays, and targeting the acyltransferase Porcupine (Porcn) without inducing Porcn destruction or mislocalization. IWR-1-endo significantly stabilized endogenous TNKS1, TNKS2 and axin 2 by inhibition of auto-PARsylation of TNKS in vivo and independent of the PARsylation activity of PARP1/2. Furthermore, IWR-1 increased expression of genes commonly expressed in cardiac mesoderm/progenitor cell and significantly improved cardiac differentiation when introduced after the application of BMP-4.
KEYWORDS: IWR-1-endo | Supplier | Wnt/TNKS inhibitor | IWR-1 | IWR1 | CAS [1127442-82-3] | DNA-RNA | TNKS1 | TNKS2 | Tankyrase | Inhibitor | catenin | parp | parsylation | axin | cardiac | differentiation | Porcupine | Porcn | | axonmedchem |
| JK184 | Axon 2654
CAS [315703-52-7]
MF C19H18N4OSMW 350.44
Purity:
100%
Soluble in DMSO and Ethanol
Description
Antagonist of Hedgehog (Hh) signaling (IC50 value of 30 nM for inhibition of Gli-dependent transcriptional activity) and a potent inhibitor of microtubule assembly that exhibits good antiproliferative activity both in vitro and in vivo. JK184 appears to act by inhibition of Adh7 (Kd value 210 nM in a assay for enzymatic oxidation of retinol).
KEYWORDS: JK184 | supplier | Hedgehog inhibitor | JK-184 | CAS [315703-52-7] | [466638-53-9] | Hedgehog | ADH | Antagonist | Hh | Smoothened | Smo | Patched | Ptch1 | Ptc | Gli | microtubules | Sonic | shh | Indian | ihh | Desert | dhh | | axonmedchem |
| MHY 553 - NSC 33005 | Axon 2814
CAS [6265-56-1]
MF C13H9NO2SMW 243.28
Purity:
98%
Soluble in DMSO
Description
MHY 553 is a PPARα agonist that improved aged-induced hepatic steatosis, in part by increasing β-oxidation signaling and decreasing inflammation in the liver. Potential pharmaceutical agent for treating hepatic steatosis in aging.
Keywords: MHY 553 | supplier | PPARα agonist | NSC 33005 | MHY553 | MHY-553 | NSC33005 | NSC-33005 | CAS [6265-56-1] | Metabolism | PPAR | Agonist | Receptors | Hepatic steatosis | | axonmedchem |
| Elafibranor - GFT505 | Axon 2727
CAS [824932-88-9]
MF C22H24O4SMW 384.49
Purity:
98%
Soluble in 0.1N NaOH(aq) and DMSO
Description
The dual PPARα/δ agonist Elafibrinor (GFT505) (EC50 values of 45 nM and 175 nM for PPARα and PPARδ, respectively) is a liver-targeted insulin-sensitizer that is a drug candidate for the treatment of type 2 diabetes, nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NAS). In animals, its protective effects are mediated by both PPAR-α-dependent and -independent mechanisms.
KEYWORDS: Elafibranor | supplier | PPAR α/δ agonist | GFT505 | GFT 505 | GFT-505 | CAS [824932-88-9] | CAS [923978-27-2] | Metabolism | PPAR | Agonist | Receptors | Insulin | Diabetes | NAFLD | NAS | Steatohepatitis | Peroxisome Proliferator-activated Receptor | | axonmedchem |
| BMS 833923 - XL 139 | Axon 2356
CAS [1059734-66-5]
MF C30H27N5OMW 473.57
Purity:
99%
Soluble in DMSO
Description
Oral, small molecule antagonist of the Hedgehog (Hh) signaling component Smoothened (SMO). Treatment with BMS 833923 leads to a decreased expression of GLI1 and PTCH1 in EGI-1 cells, reduced tumor growth in vitro, and a prolongation of survival in vivo in different human cancers. Additionally, SMO inhibition by BMS 833923 leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells (EACs).
References
Certificates
Categories
Extra info
T.L. Lin et al. Hedgehog pathway as a drug target: Smoothened inhibitors in development. Onco. Targets Ther. 2012, 5, 47-58.
J. Brechbiel et al. Crosstalk between hedgehog and other signaling pathways as a basis for combination therapies in cancer. Cancer Treat. Rev. 2014, 40, 750-759.
D. Riedlinger et al. Hedgehog pathway as a potential treatment target in human cholangiocarcinoma. J. Hepatobiliary Pancreat. Sci. 2014, 21, 607-615.
A.H. Zaidi et al. Smoothened inhibition leads to decreased proliferation and induces apoptosis in esophageal adenocarcinoma cells. Cancer Invest. 2013, 31, 480-489.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
Smoothened (SMO)
Hedgehog
F
Oral antagonist of the Hedgehog signaling component Smoothened (SMO)
Chemical name
N-(2-methyl-5-((methylamino)methyl)phenyl)-4-(4-phenylquinazolin-2-ylamino)benzamide
Parent CAS No.
[1059734-66-5]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| NVP-TNKS656 - TNKS 656 | Axon 2599
CAS [1419949-20-4]
MF C27H34N4O5MW 494.58
Purity:
99%
Soluble in DMSO
Description
Highly potent, selective and orally active tankyrase inhibitor and antagonist of Wnt pathway activity in the MMTV-Wnt1 mouse xenograft model (IC50 values 0.0155 µM and 0.0060 µM for TNKS1 and TNKS2, respectively and >5000-fold selectivity over PARP1 and PARP2).
KEYWORDS: NVP-TNKS656 | Supplier | Wnt/TNKS inhibitor | TNKS 656 | NVP-TNKS 656 | NVPTNKS656 | TNKS656 | CAS [1419949-20-4] | DNA-RNA | TNKS1 | TNKS2 | PARP | Wnt | XAV939 | KRAS-mutant | | axonmedchem |