| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| GBR 12783 dihydrochloride | Axon 1203
CAS [67469-75-4]
MF C28H32N2O.2HClMW 485.49
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective inhibitor of dopamine uptake
References
Certificates
Categories
Extra info
Bonnet and Constentin. GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo. Eur. J. Pharmacol. 1986, 121199.
Do-Rego et al. Evidence for the sequential formation of two complexes between an uptake inhibitor, GBR 12783 [1-[2-(diphenylmethoxy)ethyl]-4-(3-phenyl-2-propenyl)piperazine], and the neuronal transporter of dopamine. J. Neurochem. 1999, 72, 396.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
DRI
Unclassified
Dopamine uptake inhibitor
Chemical name
1-(2-Benzhydryloxy-ethyl)-4-((E)-3-phenyl-allyl)-piperazine dihydrochloride
Parent CAS No.
[67469-57-2]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| Bupropion hydrochloride - BW 322U | BVF 033 | Amfebutamone | Axon 1451
CAS [31677-93-7]
MF C13H18ClNO.HClMW 276.20
Purity:
99%
Soluble in water and DMSO
Description
A dopamine and noradrenaline reuptake inhibitor and nicotinic acetylcholine receptor antagonist indicated for the treatment of major depressive disorder (MDD) and for the prevention of seasonal major depressive episodes in patients with seasonal affective disorder (SAD)
References
Certificates
Categories
Extra info
RA Sweet et al. Pharmacokinetics of single-and multiple dose bupropion in elderly patients with depression. J Clin Pharmacol 1995, 35(9), 876-884.
RT Segraves et al. Evaluation of sexual functioning depressed outpatients: A double-blind comparison of sustained-release bupropion and sertraline treatment. J Clin Psychopharmacol 2000, 20(2), 122-128.
Certificate of Analysis
Material Safety Data Sheet
CNS
DRI
Unclassified
DRI and NRI; nicotinic acetylcholine receptor antagonist
Chemical name
1-(3-Chlorophenyl)-2-[(1,1-dimethylethyl)amino]-1-propanone hydrochloride
Parent CAS No.
[34911-55-2]
Order
Size
Unit Price
Stock
50 mg
€85.00
In Stock | | axonmedchem |
| Y 700 - Piraxostat | Axon 1174
CAS [206884-98-2]
MF C16H17N3O3MW 299.32
Purity:
99%
Soluble in DMSO
Description
Xanthine oxidase (XO) inhibitor
References
Certificates
Categories
Extra info
Fukunari A. et al. Y-700 [1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic Acid]: A Potent Xanthine Oxidoreductase Inhibitor with Hepatic Excretion. JPET 2004, 311, 519-528.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Xanthine Oxidase
EC 1.17.3.2
Xanthine oxidase inhibitor
Chemical name
1-[3-Cyano-4-(2,2-dimethyl-propoxy)-phenyl]-1H-pyrazole-4-carboxylic acid
Parent CAS No.
[206884-98-2]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Y 29794 tosylate | Axon 2911
CAS [143984-17-2]
MF C23H34N2OS2.C7H8O3SMW 590.86
Purity:
99%
Soluble in DMSO
Description
Y 29794 tosylate is an orally active, potent and specific prolyl endopeptidase (PPCE) inhibitor that is easily penetrable into the brain. Y-29794 tosylate selectively and competitively inhibited rat brain PPCE in a reversible manner with a Ki value of 0.95 nM. Moreover, Y 29794 tosylate exhibited potent inhibitory activity with an IC50 value of 3.0 nM for both brain crude extract and partially purified enzyme fraction.
KEYWORDS: Y 29794 tosylate | supplier | PPCE inhibitor | Y29794 tosylate | Y-29794 tosylate | CAS [143984-17-2] | [129184-48-1] | [146794-84-5] | Non Selective (Serine Peptide Bonds) | Prolyl endopeptidase | Inhibitor | Enzymes | Alzheimer's disease | | axonmedchem |
| YMU1 | Axon 2675
CAS [902589-96-2]
MF C17H22N4O4SMW 378.45
Purity:
99%
Soluble in DMSO
Description
Selective human thymidylate kinase (hTMPK; IC50 value 1.65 µM) inhibitor that lacks inhibitory effect on the activity of purified thymidine kinase 1 (TK1). YMU1 stabilizes the conformation of ligand-induced degradation (LID) region of hTMPK and blocks the catalytic site or ATP-binding site. Blocking hTMPK by YMU1 attenuates the ATP binding-induced closed conformation that is required for phosphorylation of dTMP, and sensitizes cancer cells for low-dose doxorubicin chemotherapy.
Keywords: YMU1 | supplier | TMPK inhibtor | YMU-1 | YMU 1 | CAS [902589-96-2] | Thymidylate pathway | hTMPK | Phosphotransferase | dTTP | dTMP | doxorubicin | tuberculosis | cancer | | axonmedchem |
| TEI 6720 - Febuxostat | Axon 1175
CAS [144060-53-7]
MF C16H16N2O3SMW 316.37
Purity:
99%
Soluble in DMSO
Description
A non-purine selective xanthine oxidase (XO) inhibitor
References
Certificates
Categories
Extra info
T Yamamoto et al. Effect of TEI-6720, a xanthine oxidase inhibitor, on the nucleoside transport in the lung cancer cell line A549. Pharmacology 2000, 60(1), 34-40.
K Okamoto et al. An extremely potent inhibitor of xanthine oxidoreductase. Crystal structure of the enzyme-inhibitor complex and mechanism of inhibition. J. Biol. Chem. 2003, 278(3), 1848-1855.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Xanthine Oxidase
EC 1.17.3.2
Xanthine oxidase inhibitor
Chemical name
2-(3-Cyano-4-isobutoxy-phenyl)-4-me
thyl-thiazole-5-carboxylic acid
Parent CAS No.
[144060-53-7]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Nolatrexed dihydrochloride - AG 337 | Thymitaq | Axon 2853
CAS [152946-68-4]
MF C14H12N4OS.2HClMW 357.26
Purity:
98%
Soluble in DMSO and water
Description
Nolatrexed dihydrochloride is a water soluble, lipophilic inhibitor of thymidylate synthase (Ki value of 11 nM). Nolatrexed dihydrochloride displayed non-competitive inhibition kinetics and was shown to inhibit cell growth in a panel of cell lines of murine and human origin (IC50 values between 0.39 and 6.6 µM).
KEYWORDS: Nolatrexed dihydrochloride | supplier | Thymidylate synthase inhibitor | AG 337 | Thymitaq | AG337 | AG-337 | CAS [152946-68-4] | [147149-76-6] | Deoxyuridine monophosphate (dUMP) | TYMS | Inhibitor | Enzymes | | axonmedchem |
| ZL006 | Axon 2878
CAS [1181226-02-7]
MF C14H11Cl2NO4MW 328.15
Purity:
99%
Soluble in DMSO
Description
ZL006 blocked the ischemia-induced nNOS–PSD-95 association selectively, had potent neuroprotective activity in vitro and ameliorated focal cerebral ischemic damage in mice and rats subjected to middle cerebral artery occlusion (MCAO) and reperfusion. Moreover, it readily crossed the blood-brain barrier, did not inhibit NMDAR function, catalytic activity of nNOS or spatial memory, and had no effect on aggressive behaviors.
KEYWORDS: ZL006 | supplier | nNOS-PSD-95 inhibitor | ZL 006 | ZL-006 | CAS [1181226-02-7] | Arginine, L- | NOS | Inhibitor | Enzymes | Stroke | Cerebral ischemia | Nitric oxide synthase | | axonmedchem |
| RS-1 - RAD51-Stimulatory Compound-1 | Axon 2584
CAS [312756-74-4]
MF C20H16Br2N2O3SMW 524.23
Purity:
99%
Soluble in DMSO
Description
Enhancer of CRISPR-based genome editing and homology-directed repair (HDR; RAD51). RS-1 can enhance filament stability, and stimulated hRAD51-mediated homologous strand assimilation (D-loop) activity by at least 5- to 11-fold. RS-1 acts as an allosteric regulator that locks hRAD51 in an active conformation and does so without influencing the active site for ATP hydrolysis. Treatment with RS-1 promoted significant antitumor responses in a mouse model.
KEYWORDS: RS-1 | supplier | RAD51 stimulator | RAD51-Stimulatory Compound-1 | RS1 | CAS [312756-74-4] | DNA-RNA | RAD51 | Stimulator | CRISPR | genome editing | homology-directed repair | HDR | filaments | Cas9 | | axonmedchem |
| RAD51 inhibitor B02 | Axon 1911
CAS [1290541-46-6]
MF C22H17N3OMW 339.39
Purity:
98%
Soluble in DMSO
Description
Specific and cell-permeable RAD51 inhibitor; BO2 specifically inhibits the DNA strand exchange activity of human RAD51 (IC50 = 27.4 μM). It disrupts RAD51 binding to DNA, increasing cell sensitivity to DNA damage
References
Certificates
Categories
Extra info
F Huang et al. Identification of Specific Inhibitors of Human RAD51 Recombinase Using High-Throughput Screening. ACS Chem. Biol. 2011, 6, 628-635.
F Huang et al. Inhibition of Homologous Recombination in Human Cells by Targeting RAD51 Recombinase. J. Med. Chem. 2012, 55, 3011−3020
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
RAD51
DNA-damage Response
EC 3.1.22.4
Inhibitor of RAD51
Chemical name
(E)-3-benzyl-2-(2-(pyridin-3-yl)vinyl)quinazolin-4(3H)-one
Parent CAS No.
[1290541-46-6]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| RI-1 | Axon 1885
CAS [415713-60-9]
MF C14H11Cl3N2O3MW 361.61
Purity:
99%
Soluble in DMSO
Description
Specific inhibitor of the central recombination protein RAD51; a useful tool for investigations on mechanisms of DNA repair
References
Certificates
Categories
Extra info
B Budke et al. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012, 40(15), 7347-7357.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
RAD51
DNA-damage Response
EC 3.1.22.4
Inhibitor of the central recombination protein RAD51
Chemical name
3-chloro-1-(3,4-dichlorophenyl)-4-morpholino-1H-pyrrole-2,5-dione
Parent CAS No.
[415713-60-9]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Luciferin, D- - Firefly Luciferin | Axon 2494
CAS [2591-17-5]
MF C11H8N2O3S2MW 280.32
Purity:
98%
Optical purity:
Optically pure
Soluble in 0.1N NaOH(aq) and DMSO
Description
Substrate of firefly luciferase. Bioluminescent compound that may be used for in vivo bioluminescence imaging (BLI)
References
Certificates
Categories
Extra info
A. Sato et al. In vivo bioluminescence imaging. Comp Med. 2004 Dec;54(6):631-4.
I. Presiado et al. Excited-state intermolecular proton transfer of firefly luciferin III. Proton transfer to a mild base. J Phys Chem A. 2010 Dec 30;114(51):13337-46.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Proteins
Luciferase
EC 1.13.12.7
Natural substrate of firefly luciferase. Compound for bioluminescence imaging (BLI)
Chemical name
(S)-2-(6-hydroxybenzo[d]thiazol-2-yl)-4,5-dihydrothiazole-4-carboxylic acid
Parent CAS No.
[2591-17-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| Dansyl-PEG-phenylboronic acid | Axon 2257
CAS [N.A.]
MF C30H41BN4O9SMW 644.54
Purity:
98%
Soluble in 0.1N HCl(aq), MeOH and DMSO
Description
Dansylamide functionalized PEG-phenylboronic acid for the use of palladium-catalyzed oxidative Heck reaction to protein-bound alkenes and Suzuki-Miyaura cross coupling for labeling of protein bound phenylhalides in high yields and with excellent chemoselectivity. Reagent for bio-orthogonal protein-ligation.*Sold in collaboration with RuG (University of Groningen)
References
Certificates
Categories
Extra info
ME Ourailidou et al. Aqueous oxidative Heck reaction as a protein-labeling strategy. Chembiochem. 2014, 15, 209-212.
F D'Hooge et al. Biotinylated boronic acid fluorophore conjugates: Quencher elimination strategy for imaging and saccharide detection. RSC Adv. 2012, 2, 3274-3280.
Chalker et al. A Convenient Catalyst for Aqueous and Protein Suzuki-Miyaura Cross-Coupling J. Am. Chem. Soc. 2009, 131, 16346-16347
C.D. Spicer et al. Palladium-mediated site-selective Suzuki-Miyaura protein modification at genetically encoded aryl halides. Chem. Commun. 2011, 47, 1698-700
C.D. Spicer et al. Palladium-mediated cell-surface labeling. J. Am. Chem. Soc. 2012, 134(2), 800-3.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Proteins
RuG Collaboration Products
Dansylamide functionalized PEG-phenylboronic acid; Protein labeling reagent
Chemical name
3-(1-(5-(dimethylamino)naphthalene-1-sulfonamido)-13-oxo-3,6,9-trioxa-12-azahexadecanamido)phenylboronic acid
Source information
Sold in collaboration with RuG (University of Groningen)
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| Biotinyl-phenylboronic acid | Axon 2256
CAS [N.A.]
MF C16H22BN3O4SMW 363.24
Purity:
99%
Soluble in 0.1N NaOH(aq), MeOH and DMSO
Description
Biotin functionalized arylboronic acid for the use of palladium-catalyzed oxidative Heck reaction to protein-bound alkenes and Suzuki-Miyaura cross-coupling for labeling of protein bound phenylhalides in high yields and with excellent chemoselectivity. Reagent for bio-orthogonal protein-ligation. Signal enhancement with streptavidin-HRP.*Sold in collaboration with RuG (University of Groningen)
References
Certificates
Categories
Extra info
ME Ourailidou et al. Aqueous oxidative Heck reaction as a protein-labeling strategy. Chembiochem. 2014, 15, 209-212.
F D'Hooge et al. Biotinylated boronic acid fluorophore conjugates: Quencher elimination strategy for imaging and saccharide detection. RSC Adv. 2012, 2, 3274-3280.
Chalker et al. A Convenient Catalyst for Aqueous and Protein Suzuki-Miyaura Cross-Coupling J. Am. Chem. Soc. 2009, 131, 16346-16347
C.D. Spicer et al. Palladium-mediated site-selective Suzuki-Miyaura protein modification at genetically encoded aryl halides. Chem. Commun. 2011, 47, 1698-700
C.D. Spicer et al. Palladium-mediated cell-surface labeling. J. Am. Chem. Soc. 2012, 134(2), 800-3.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Proteins
RuG Collaboration Products
Biotinylated arylboronic acid for bio-orthogonal chemistry
Chemical name
3-(5-(2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)pentanamido)phenylboronic acid
Source information
Sold in collaboration with RuG (University of Groningen)
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Aminoacridone, 2- | Axon 1878
CAS [27918-14-5]
MF C13H10N2OMW 210.23
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Excellent derivatisation reagent tuned toward the mild labeling of malondialdehyde and subsequent identification by fluorescence. Derivatisation can be carried out in aqueous citrate buffer at 40 °C. Also as Fluorescent label for glycans and saccharides
References
Certificates
Categories
Extra info
M Giera et al. Mild and selective labeling of malondialdehyde with 2-aminoacridone: assessment of urinary malondialdehyde levels. Analyst. 2011, 136(13), 2763-9.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Glycans
Malondialdehyde
Labeling agent of malondialdehyde (Fluorescent)
Chemical name
2-aminoacridin-9(10H)-one
Parent CAS No.
[27918-14-5]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| APEBA, 4- - VUF 10996 | Axon 1877
CAS [1226984-28-6]
MF C18H25Br3N2OMW 525.12
Purity:
99%
Soluble in water and DMSO
Description
Excellent derivatisation reagent for aldehydes and carboxylic acids. Very mild derivatisation conditions. Selectivity for aldehydes or carboxylic acids is obtained by changing co-reagent. In addition to the retained features of the 1st generation reagent 4-APC, 4-APEBA and its adducts contain additional unique properties (Br-isotope identifier, specific bromophenethyl fragmentation, increased lipophilicity).*Sold in collaboration with VU (VU University Amsterdam).
References
Certificates
Categories
Extra info
Kretschmer A, Giera M, Wijtmans M, de Vries L, Lingeman H, Irth H, Niessen WM. Derivatization of carboxylic acids with 4-APEBA for detection by positive-ion LC-ESI-MS(/MS) applied for the analysis (...). J Chromatogr B 2011, 879(17-18), 1393-1401.
Eggink M, Wijtmans M, Kretschmer A, Kool J, Lingeman H, de Esch IJ, Niessen WM, Irth H. Targeted LC-MS derivatization for aldehydes and carboxylic acids with a new derivatization agent 4-APEBA. Anal Bioanal Chem. 2010, 397(2), 665-675.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Aldehydes
Carboxylic acids
VU Collaboration Products
Derivatisation reagent for aldehydes and carboxylic acids
Chemical name
4-(2-((4-bromophenethyl)dimethylammonio)ethoxy)benzenaminium bromide
Source information
Sold in collaboration with VU (VU University Amsterdam).
Parent CAS No.
[1227040-19-8]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| APC, 4- - VUF 11000 | Axon 1876
CAS [1076196-38-7 ]
MF C11H20Br2N2OMW 356.10
Purity:
99%
Soluble in DMSO
Description
Excellent derivatisation reagent for aldehydes, yielding adducts with LC-MS-tuned identifiers and properties. Very mild derivatisation conditions (NaBH3CN, water, pH 5.7, 4 °C). Attractive selectivity profile (including over ketones) and specific fragmentation properties in MS/MS profiling sensitivity and specificity.* Sold in collaboration with VU (VU University Amsterdam)
References
Certificates
Categories
Extra info
Eggink M, Charret S, Wijtmans M, Lingeman H, Kool J, Niessen WM, Irth H. Development of an on-line weak-cation exchange liquid chromatography-tandem mass spectrometric method for (...). J Chromatogr B 2009, 877(31), 3937-3945.
Eggink M, Wijtmans M, Ekkebus R, Lingeman H, de Esch IJ, Kool J, Niessen WM, Irth H. Development of a selective ESI-MS derivatization reagent: synthesis and optimization for the analysis of aldehydes (...). Anal Chem. 2008, 80(23), 9042-9051.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Aldehydes
VU Collaboration Products
Derivatisation reagent for aldehydes
Chemical name
4-(2-(trimethylammonio)ethoxy)benzenaminium bromide
Source information
Sold in collaboration with VU (VU University Amsterdam)
Parent CAS No.
[76201-92-8]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| PKG drug G1 sodium salt | Axon 2905
CAS [N.A.]
MF C13H10N3NaOSMW 279.29
Purity:
98%
Soluble in water and DMSO
Description
PKG drug G1 sodium salt has been shown to induce the oxidative activation of protein kinase G Iα, which in vivo results in dilation of blood vessel and blood pressure lowering; an antihypertensive.
The parent molecule is also available as Axon 2232.
* Developed and sold in collaboration with KCL (King's College of London).
KEYWORDS: PKG drug G1 sodium salt | supplier | PKG Iα inducer | CAS [N.A.] | [374703-78-3] | Non Selective (Phosphorylation Substrates) | PKG | Inducer | Enzymes | Antihypertension | | axonmedchem |
| P7C3 | Axon 2602
CAS [301353-96-8]
MF C21H18Br2N2OMW 474.19
Purity:
99%
Soluble in DMSO
Description
Orally bioavailable and brain penetrant proneurogenic and neuroprotective compound that activates NAMPT (nicotinamide phosphoribosyltransferase). P7C3 exerts antidepressant efficacy in mice by increasing hippocampal neurogenesis, and improves cognitive function in aged rats and increases neuronal survival in mouse models of Parkinson's disease (PD) and amyotrophic lateral sclerosis (ALS).
KEYWORDS: P7C3 | supplier | NAMPT activator | CAS [301353-96-8] | Nicotinamide D-ribonucleotide | nicotinamide phosphoribosyltransferase | orally bioavailable | brain penetrant | Parkinson's | amyotrophic lateral sclerosis | ALS | proneurogenic | neuroprotective | antidepressant | neurogenesis | cognitive function | neuronal survival | | axonmedchem |
| PKG drug G1 | Axon 2232
CAS [374703-78-3]
MF C13H11N3OSMW 257.31
Purity:
99%
Soluble in DMSO
Description
PKG drug G1 has been shown to induce the oxidative activation of protein kinase G Iα, which in vivo results in dilation of blood vessel and blood pressure lowering; an antihypertensive.
The sodium salt form is also available as Axon 2905.
* Developed and sold in collaboration with KCL (King's College of London).
KEYWORDS: PKG drug G1 | supplier | PKG Iα inducer | CAS [374703-78-3] | Non Selective (Phosphorylation Substrates) | PKG | Inducer | Enzymes | Antihypertension | | axonmedchem |
| STF 118804 | Axon 2253
CAS [894187-61-2]
MF C25H23N3O4SMW 461.53
Purity:
98%
Soluble in DMSO
Description
Highly specific, next-generation NAMPT inhibitor, that reduces the viability of most B-ALL cell lines with high potency demonstrating IC50 values in the low nanomolar range, and improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia. Additionally, STF 118804 induces leukemia cell apoptosis without antecedent cell cycle arrest, and targets leukemia stem cells.
KEYWORDS: STF 118804 | supplier | NAMPT inhibitor | STF118804 | CAS [894187-61-2] | Nicotinamide D-ribonucleotide | NAD | NAD+ | apoptosis | leukemia | cell cycle | arrest | stem cells | | axonmedchem |
| FK 866 hydrochloride - K 22.175 hydrochloride | Axon 1546
CAS [658084-64-1]
MF C24H29N3O2.HClMW 427.97
Purity:
99%
Soluble in water and DMSO
Description
Highly specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT); NAD biosysthesis inhibitor; Tumor cell apoptosis agent (see also Axon 1279)
References
Certificates
Categories
Extra info
M. Hasmann and I. Schemainda, FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis. Cancer Res. 2003, 63, 7436-7442.
A Pogrebniak et al. Chemopotentiating effects of a novel NAD biosynthesis inhibitor, FK866, in combination with antineoplastic agents. Eur. J. Med. Res. 2006, 11(8), 313-321.
K Holen et al. The pharmacokinetics, toxicities, and biologic effects of FK866, a nicotinamide adenine dinucleotide biosynthesis inhibitor. Invest. New Drugs. 2008, 26(1), 45-51.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Diabetes & Metabolism
NAMPT
EC 2.4.2.12
NAMPT inhibitor
Chemical name
(E)-N-[4-(1-Benzoyl-piperidin-4-yl)-butyl]-3-pyridin-3-yl-acrylamide hydrochloride
Parent CAS No.
[658084-64-1]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| FK 866 - Daporinad | APO 866 | Axon 1279
CAS [658084-64-1]
MF C24H29N3O2MW 391.51
Purity:
99%
Soluble in 0.1N HCl(aq), DMSO, and Ethanol
Description
Highly specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT); NAD biosynthesis inhibitor; Tumor cell apoptosis agent (see also Axon 1546)
KEYWORDS: FK 866 | supplier | NAMPT inhibitor | Daporinad | APO 866 | FK866 | APO866 | FK-866 | APO-866 | CAS [658084-64-1] | Nicotinamide D-ribonucleotide | phosphoribosyltransferase | NAD biosynthesis inhibitor | Tumor cell | apoptosis | | axonmedchem |
| Balicatib - AAE 581 | Axon 2154
CAS [354813-19-7]
MF C23H33N5O2MW 411.54
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of the osteoclastic enzyme cathepsin K
References
Certificates
Categories
Extra info
C Jerome et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2011, 22(12), 3001-3011.
TM Ruenger et al. Morphea-like skin reactions in patients treated with the cathepsin K inhibitor balicatib. J. Am. Acad. Dermatol. 2012, 66(3), e89-e96.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Miscellaneous
Cathepsin-K
EC 3.4.22.8
Selective inhibitor of cathepsin K
Chemical name
N-(1-(cyanomethylcarbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
Parent CAS No.
[354813-19-7]
Order
Size
Unit Price
Stock
2 mg
€80.00
In Stock | | axonmedchem |
| AZD 1208 | Axon 2795
CAS [1204144-28-4]
MF C21H21N3O2SMW 379.48
Purity:
98%
Optical purity:
optically pure
Soluble in DMSO
Description
AZD 1208 is a pan-Pim kinase inhibitor (IC50 values of 0.4 nM, 5.0 nM and 1.9 nM for Pim-1, Pim-2 and Pim-3, respectively) which does not inhibit FLT3. AZD 1208 treatment resulted in growth inhibition and cell size reduction in AML cell lines including FLT3-WT (OCI-AML-3, KG-1a, MOLM-16) and FLT3-ITD mutated (MOLM-13, MV-4-11).
KEYWORDS: AZD 1208 | supplier | PIM inhibitor | AZD1208 | AZD-1208 | CAS [1204144-28-4] | Non Selective (Phosphorylation Substrates) | PIM | Inhibitor | Enzymes | AML | | axonmedchem |
| ONO 5334 | Axon 2156
CAS [868273-90-9]
MF C21H34N4O4SMW 438.58
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and orally available inhibitor of cathepsin K (Ki values of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat respectively). ONO 5334 dose depedently suppresses human osteoclast-mediated bone resorption in vitro, and reduced PTHrP-induced increase in plasma calcium with significant effect (86% reduction) after oral administration in TPTX pretreated rats.
References
Certificates
Categories
Extra info
R. Eastell et al. Effect of ONO-5334 on Bone Mineral Density and Biochemical Markers of Bone Turnover in Postmenopausal Osteoporosis: 2-Year Results From the OCEAN Study. J. Bone Miner Res. 2014, 29, 458-466.
Y. Ochi et al. Effects of ONO-5334, a novel orally-active inhibitor of cathepsin K, on bone metabolism. Bone. 2011, 49, 1351-1356.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Miscellaneous
Cathepsin-K
EC 3.4.22.8
Potent and orally available inhibitor of cathepsin K
Chemical name
N-((R)-3-((Z)-2-((R)-3,4-dimethylthiazolidin-2-ylidene)hydrazinyl)-2,3-dioxo-1-(tetrahydro-2H-pyran-4-yl)propyl)cycloheptanecarboxamide
Parent CAS No.
[868273-90-9]
Order
Size
Unit Price
Stock
2 mg
€110.00
In Stock | | axonmedchem |
| CX 6258 hydrochloride | Axon 2305
CAS [1353859-00-3]
MF C26H24ClN3O3.HClMW 498.40
Purity:
99%
Soluble in DMSO
Description
Potent, selective, and orally efficacious pan-Pim kinases inhibitor (IC50 values 5 nM, 25 nM, and 16 nM for Pim-1, Pim-2, and Pim-3 respectively) with 5-40 fold selectivity over Flt-3 (IC50 values 0.134 μM).CX 6258 exhibited dose dependent efficacy in a mouse MV-4-11 xenograft study, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI, and was well tolerated throughout the study.
References
Certificates
Categories
Extra info
M. Haddach et al. Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett. 2011, 3, 135-139.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Immunology
JAK-STAT
EC 2.7.11.1
PIM
Pim kinase inhibitor
Chemical name
(E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one hydrochloride
Parent CAS No.
[1202916-90-2]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| SMI 4a - Pim inhibitor 4a | Axon 1923
CAS [438190-29-5]
MF C11H6F3NO2SMW 273.23
Purity:
98%
Soluble in DMSO
Description
ATP-competitive and selective inhibitor of Pim kinases, with IC50 values of 24 and 100 nM for Pim-1 and Pim-2 respectively. SMI-4a inhibits prostate cancer cell growth and induce G1 phase cell-cycle arrest in precursor T-cell lymphoblastic leukemia/lymphoma cell lines
References
Certificates
Categories
Extra info
Z Xia et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J. Med. Chem. 2009, 52(1), 74-86.
YW Lin et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood. 2010, 115(4), 824-833.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Immunology
JAK-STAT
EC 2.7.11.1
PIM
ATP-competitive and selective inhibitor of Pim kinases
Chemical name
(Z)-5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione
Parent CAS No.
[438190-29-5]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SGI 1776 free base | Axon 1633
CAS [1025065-69-3]
MF C20H22F3N5OMW 405.42
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
A potent and selective inhibitor of Pim kinases, inducing apoptosis and cell cycle arrest, thereby causing a reduction in phospho-BAD levels and enhancement of mTOR inhibition in vitro. Most notably, SGI-1776 induced significant tumor regression in MV-4-11 (AML) and MOLM-13 (AML) xenograft models
References
Certificates
Categories
Extra info
LS Chen et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in CLL lymphocytes. Blood, 2009, 114 (19), 4150-4157.
SM Mumenthaler et al. Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. Mol. Cancer Ther. 2009, 8(10), 2882-2893.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Immunology
JAK-STAT
EC 2.7.11.1
PIM
Pim kinase inhibitor
Chemical name
N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine
Parent CAS No.
[1025065-69-3]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| MK 0822 - Odanacatib | Axon 1771
CAS [603139-19-1]
MF C25H27F4N3O3SMW 525.56
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and selective inhibitor of cathepsin K (CTSK or Cat K)
References
Certificates
Categories
Extra info
CL Le Gall et al. Cathepsin K inhibitors as treatment of bone metastasis. Curr. Opin. Support. Palliat. Care. 2008, 2(3), 218.
JY Gauthier et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg. Med. Chem. Lett. 2008, 18(3), 923–928.
EM Lewiecki. Odanacatib, a cathepsin K inhibitor for the treatment of osteoporosis and other skeletal disorders associated with excessive bone remodeling. IDrugs. 2009, 12(12), 799-809.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Miscellaneous
Cathepsin-K
EC 3.4.22.8
Inhibitor of cathepsin K
Chemical name
(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Parent CAS No.
[603139-19-1]
Order
Size
Unit Price
Stock
2 mg
€80.00
In Stock | | axonmedchem |
| NSC 756093 | Axon 2393
CAS [1629908-92-4]
MF C20H19NO4MW 337.37
Purity:
99%
Soluble in DMSO
Description
Potent in vitro inhibitor of GBP1:PIM1 interaction (65% inhibition of interaction at 100 nM) with activity in paclitaxel resistant cells.
References
Certificates
Categories
Extra info
M. Andreoli et al. Identification of the first inhibitor of the GBP1:PIM1 interaction. Implications for the development of a new class of anticancer agents against paclitaxel resistant cancer cells. J Med Chem. 2014 Oct 9;57(19):7916-32.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
GBP1
EC 3.6.5.6
Potent in vitro inhibitor of GBP1:PIM1 interaction
Chemical name
4-(2-hydroxyethyl)-6-methoxy-9-phenyl-4,9-dihydrofuro[3,4-b]quinolin-1(3H)-one
Parent CAS No.
[1629908-92-4]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| CGP 57380 | Axon 1611
CAS [522629-08-9]
MF C11H9FN6MW 244.23
Purity:
99%
Soluble in DMSO
Description
Inhibitor of MAP-kinase interacting kinase-1 (Mnk1, MKNK1) that displays selectivity over p38, JNK1, ERK1, ERK2, PKC and c-src family kinases.
KEYWORDS: CGP 57380 | supplier | Mnk1 inhibitor | CGP57380 | CGP-57380 | CAS [522629-08-9] | DNA-RNA | Mnk1 | Inhibitor | Enzymes | | axonmedchem |
| CCG 50014 | Axon 1931
CAS [883050-24-6]
MF C16H13FN2O2SMW 316.35
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of regulator of G-protein signaling (RGS) proteins. It has an IC50 value of 30 nM for RGS4 and 20 fold selectivity for RGS4 over other RGS proteins
References
Certificates
Categories
Extra info
LL Blazer et al. A nanomolar-potency small molecule inhibitor of regulator of G-protein signaling proteins. Biochemistry 2011, 50(15), 3181-3192.
EM Turner et al. Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins. ACS Med Chem Lett. 2012, 3(2), 146-150.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
RGS4
EC 3.6.5.1
Inhibitor of RGS proteins (RGS4 selective)
Chemical name
4-(4-fluorobenzyl)-2-p-tolyl-1,2,4-thiadiazolidine-3,5-dione
Parent CAS No.
[883050-24-6]
Order
Size
Unit Price
Stock
10 mg
€99.00
In Stock | | axonmedchem |
| CBR 5884 | Axon 2585
CAS [681159-27-3]
MF C14H12N2O4S2MW 336.39
Purity:
99%
Soluble in DMSO
Description
Noncompetitive inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH; IC50 value 33 µM) with selective toxicity towards cancer cell lines with high serine biosynthetic activity. CBR-5884 shows no inhibitory effect on two other NAD+-dependent dehydrogenases, lactate dehydrogenase (LDH) and MDH1A. A useful tool to study the biology of de novo serine synthesis enabling preclinical evaluation of PHGDH as a target in cancer.
KEYWORDS: CBR 5884 | supplier | PHGDH inhibitor | CBR5884 | CAS [681159-27-3] | 3-phosphoglycerate | PHGDH | dehydrogenase | breast | cancer | serine biosynthesis | NAD+ dependent | | axonmedchem |
| CAIX Inhibitor S4 | Axon 2662
CAS [1330061-67-0]
MF C15H17N3O4SMW 335.38
Purity:
99%
Soluble in DMSO
Description
S4 is a carbonic anhydrase (CA) IX and XII inhibitor (Ki values 7 nM and 2 nM, respectively) and showed a positive response in in vitro assays for tumor cell migration and spreading. Moreover, CAIX inhibitor S4 effectively inhibited the spontaneous metastasis formation in MDA-MB-231 xenografts. | | axonmedchem |
| BTZ043 | Axon 2698
CAS [1161233-85-7]
MF C17H16F3N3O5SMW 431.39
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO
Description
Antimycobacterial agent that kills Mycobacterium tuberculosis (MIC values 2.3 nM and 9.2 nM against M. tuberculosis H37Rv and M. smegmatis, respectively) in vitro, ex vivo, and in mouse models of TB through inhibition of decaprenylphosphoryl-b-D-ribose 2′-epimerase (DprE1).
KEYWORDS: BTZ043 | supplier | DprE1 inhibitor | BTZ-043 | BTZ 043 | BTZ-10526043 | BTZ 10526043 | CAS [1161233-85-7] | Decaprenylphosphoryl-beta-D-ribofuranose (DPR) | DprE | Inhibitor | Enzymes | | axonmedchem |
| NCT-503 | Axon 2623
CAS [1916571-90-8]
MF C20H23F3N4SMW 408.48
Purity:
98%
Soluble in 0.1N HCl (aq) and DMSO
Description
Non-competitive PHGDH inhibitor (IC50 value 2.5 µM) that reduces the production of glucose-derived serine in cells and suppresses the growth of PHGDH-dependent cancer cells in culture and in orthotopic xenograft tumors.
KEYWORDS: NCT-503 | supplier | PHGDH inhibitor | NCT503 | NCT 503 | CAS [1916571-90-8] | 3-phosphoglycerate | 3-PG | serine | cancer | NSCLC | phosphoglycerate dehydrogenase | | axonmedchem |
| PBTZ169 | Axon 2626
CAS [1377239-83-2]
MF C20H23F3N4O3SMW 456.48
Purity:
100%
Soluble in DMSO and Ethanol
Description
Potent irreversible DprE1 inhibitor (MIC value <0.19 ng/mL and <0.004 µM against M. tuberculosis H37Ra) with improved stability against nitroreductase metabolism, and good efficacy at lower concentrations in the murine model of chronic tuberculosis (TB); an attractive drug candidate to treat TB in humans. The combination of PBTZ169, BDQ and pyrazinamide was found to be more efficacious than the standard three drug treatment in a murine model of chronic disease.
KEYWORDS: PBTZ169 | supplier | DprE1 inhibitor | PBTZ-169 | PBTZ 169 | CAS [1377239-83-2] | DPR | DprE | tuberculosis | TB | mycobacterium | flavo-enzyme | cell wall | biosynthesis | benzothiazinone | epimerase | Decaprenylphosphoryl-beta-D-ribofuranose | | axonmedchem |
| CX 4945 hydrochloride - Silmitasertib hydrochloride | Axon 1965
CAS [N.A.]
MF C19H12ClN3O2.HClMW 386.23
Purity:
98%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Orally available, potent and selective casein kinase 2 (CK2) inhibitor
References
Certificates
Categories
Extra info
A Siddiqui-Jain et al. CX-4945, an Orally Bioavailable Selective Inhibitor of Protein Kinase CK2, Inhibits Prosurvival and Angiogenic Signaling and Exhibits Antitumor Efficacy. Cancer Res. 2010, 70, 10288-10298.
AD Ferguson et al. Structural basis of CX-4945 binding to human protein kinase CK2. FEBS Lett. 2011, 585(1), 104-110.
F Pierre et al. Pre-clinical characterization of CX-4945, a potent and selective small molecule inhibitor of CK2 for the treatment of cancer. Mol. Cell Biochem. 2011, 356(1-2), 37-43.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
EC 2.7.11.1
CK
Inhibitor of Casein kinase 2 (CK2)
Chemical name
5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid hydrochloride
Parent CAS No.
[1009820-21-6]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| cPEPCK inhibitor | Axon 1165
CAS [628279-07-2]
MF C25H26FN5O3MW 463.50
Purity:
98%
Soluble in DMSO
Description
The first GTP-competitive inhibitor of human cytosolic phosphoenolpyruvate carboxykinase (PEPCK or cPEPCK) with low submicromolar IC50 values.
KEYWORDS: cPEPCK inhibitor | supplier | cPEPCK inhibitor | CAS [628279-07-2] | Gluconeogenesis | PEPCK | GTP-competitive | human | cytosolic | phosphoenolpyruvate carboxykinase | glucose homeostasis | Type 2 | diabetes | | axonmedchem |
| Dorzolamide hydrochloride | Axon 1517
CAS [130693-82-2]
MF C10H17ClN2O4S3MW 360.90
Purity:
99%
Soluble in water and DMSO
Description
A carbonic anhydrase inhibitor; antiglaucoma agent, used to lower increased intraocular pressure in open-angle glaucoma and ocular hypertension
References
Certificates
Categories
Extra info
C Plummer et al. Comparison of the effects of topical administration of a fixed combination of dorzolamide-timolol to monotherapy with timolol or dorzolamide on IOP, pupil size, and heart rate in glaucomatous dogs. Vet. Ophthalmol. 2006, 9(4), 245–249.
S Grover et al. Topical dorzolamide for the treatment of cystoid macular edema in patients with retinitis pigmentosa. Am. J. Ophthalmol. 2006, 141(5), 850–858.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Diabetes & Metabolism
Miscellaneous
Carbonic Anhydrase
EC 4.2.1.1.
Carbonic anhydrase inhibitor
Chemical name
(4S,6S)-4-(ethylamino)-5,6-dihydro-6-methyl-, 7,7-dioxide 4H-Thieno[2,3-b]thiopyran-2-sulfonamide hydrochloride
Parent CAS No.
[120279-96-1]
Order
Size
Unit Price
Stock
10 mg
€70.00
In Stock | | axonmedchem |
| LH 846 | Axon 2297
CAS [639052-78-1]
MF C16H13ClN2OSMW 316.81
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of CK1δ ( IC50 values of 2.5 mM, 290 nM, and 1.3 mM for CK1α, CK1δ, and CK1ε, respectively) that showed no inhibitory effect on CK2. LH 846 modulates circadian rhythms through phosphorylation of the period protein with a significant effect on circadian period length (10 h) with minimal effect on the amplitude of both Per2-dLuc and Bmal1-dLuc rhythms in U2OS cells.
References
Certificates
Categories
Extra info
J.W. Lee et al. A small molecule modulates circadian rhythms through phosphorylation of the period protein. Angew. Chem. Int. Ed. Engl. 2011, 50, 10608-10611.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
EC 2.7.11.1
CK
Inhibitor of Casein kinase 1 (CK1δ)
Chemical name
N-(5-chloro-6-methylbenzo[d]thiazol-2-yl)-2-phenylacetamide
Parent CAS No.
[639052-78-1]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| TTP 22 | Axon 1854
CAS [329907-28-0]
MF C16H14N2O2S2MW 330.42
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent and ATP-competitive casein kinase 2 (CK2) inhibitor (IC50 = 0.1 μM, Ki = 40 nM)
References
Certificates
Categories
Extra info
AG Golub et al. Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2. Eur. J. Med. Chem. 2011, 46(3), 870-6.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
EC 2.7.11.1
CK
Inhibitor of Casein kinase 2 (CK2)
Chemical name
3-(5-p-tolylthieno[2,3-d]pyrimidin-4-ylthio)propanoic acid
Parent CAS No.
[329907-28-0]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| SR 3029 | Axon 2547
CAS [1454585-06-8]
MF C23H19F3N8OMW 480.45
Purity:
99%
Soluble in DMSO
Description
A potent, highly specific CK1δ/CK1ε inhibitor (IC50 values 44 nM and 260 nM for CK1δ, and CK1ε, respectively), that selectively inhibits breast cancer cell growth and survival. SR-3029 exhibits in vitro and in vivo PK properties suitable for use in xenograft studies of human cancers, including brain cancers.
KEYWORDS: SR 3029 | supplier | CK1δ/CK1ε inhibitor | CK1 inhibitor | SR3029 | CAS [1454585-06-8] | casein kinase | CK1 | Inhibitor | breast cancer | brain cancer | Wnt | catenin | signaling | HER2 | FLT3 | CK1-delta | CK1-epsilon | | axonmedchem |
| CK2 inhibitor 10 | Axon 2202
CAS [1361229-76-6]
MF C18H14N2O4SMW 354.38
Purity:
99%
Soluble in DMSO
Description
Potent and ATP-competitive inhibitor of protein kinase (CK2; IC50 values of 32 nM and 46 nM for CK2α and CK2α' respectively). At 0.30 μM, compound 10 exhibited a >50% inhibitory effect against 9 out of 70 other kinases besides CK2α and CK2α′, while at 30 nM >75% inhibition was observed for two other kinases (DYRK1B and FLT3) only. It exhibited potent cytotoxicity towards lung cancer cells A549, colorectal cancer cells HCT-116, and breast cancer cells MCF-7.
References
Certificates
Categories
Extra info
Z. Hou et al. Structure-based design of novel potent protein kinase CK2 (CK2) inhibitors with phenyl-azole scaffolds. J. Med. Chem. 2012, 55, 2899-2903.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
EC 2.7.11.1
CK
Potent and ATP-competitive inhibitor of CK2
Chemical name
4-(2-(4-methoxybenzamido)thiazol-5-yl)benzoic acid
Parent CAS No.
[1361229-76-6]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| PF 4800567 | Axon 1792
CAS [1188296-52-7]
MF C17H18ClN5O2MW 359.81
Purity:
98%
Soluble in DMSO
Description
Potent and selective casein kinase 1ε (Csnk1e or CK-1ε) inhibitor (IC50: 32 nM) with >20-fold selectivity over CK 1δ
References
Certificates
Categories
Extra info
KM Walton et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J. Pharmacol. Exp. Ther. 2009, 330(2), 430-439.
QJ Meng et al. Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes. Proc. Natl. Acad. Sci. USA. 2010, 107(34), 15240-15245.
CD Bryant et al. Csnk1e is a Genetic Regulator of Sensitivity to Psychostimulants and Opioids. Neuropsychopharmacology. 2011, 37, 1026-1035.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Wnt-β-Catenin
EC 2.7.11.1
CK
Inhibitor of Casein kinase 1 (CK1-ε)
Chemical name
3-((3-chlorophenoxy)methyl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
Parent CAS No.
[1188296-52-7]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| EN460 - ERO1 Inhibitor II | Axon 2737
CAS [496807-64-8]
MF C22H12ClF3N2O4MW 460.79
Purity:
99%
Soluble in DMSO
Description
EN460, an inhibitor of endoplasmic reticulum oxidation 1 (ERO1), interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation (IC50 value of 1.9 μM). Despite rapid and promiscuous reactivity with thiolates, EN460 exhibits selectivity for ERO1.
KEYWORDS: EN460 | supplier | ERO1 inhibitor | ERO1 Inhibitor II | EN 460 | EN-460 | CAS [496807-64-8] | Protein Disulfide Isomerase (PDI) | ERO1 | Inhibitor | Enzymes | Endoplasmic Reticulum Oxidation | | axonmedchem |
| Defactinib - VS 6063 | PF 04554878 | Axon 2574
CAS [1073154-85-4]
MF C20H21F3N8O3SMW 510.49
Purity:
98%
Soluble in DMSO
Description
Orally available second-generation inhibitor of focal adhesion kinase (FAK) and proline-rich tyrosine kinase-2 (PYK2) with an acceptable safety profile in clinical trials (IC50 values 0.6 nM for each kinase, and >100-fold greater selectivity for FAK and PYK2 than for other, non-target kinases). Structurally closely related to PF 431396 (Axon 2107).
KEYWORDS: Defactinib | supplier | FAK/PYK2 inhibitor | VS 6063 | PF 04554878 | PF04554878 | VS6063 | PF4554878 | CAS [1073154-85-4] | [1073160-26-5] | Phosphorylation | FAK | PYK2 | Inhibitor | focal adhesion kinase | proline-rich tyrosine kinase-2 | solid | tumor | malignancies | prostate cancer | | axonmedchem |
| DC 838 | Axon 1166
CAS [508186-08-1]
MF C27H29N5O4MW 487.55
Purity:
99%
Soluble in DMSO
Description
Potent human cyclophilin A (CypA) inhibitor
References
Certificates
Categories
Extra info
J Li et al. One novel quinoxaline derivative as a potent human cyclophilin A inhibitor shows highly inhibitory activity against mouse spleen cell proliferation. Bioorg. Med. Chem. 2006, 14(16), 5527-5534.
Certificate of Analysis
Material Safety Data Sheet
Immunology
Pain & Inflammation
CypA
EC 5.2.1.8
CypA inhibitor
Chemical name
Piperidine-1,3-dicarboxylic acid 3-diethylamide 1-[(2,3-di-furan-2-yl-quinoxalin-6-yl)-amide]
Parent CAS No.
[508186-08-1]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| PND 1186 - SR 2516 | VS 4718 | Axon 2459
CAS [1061353-68-1]
MF C25H26F3N5O3MW 501.50
Purity:
100%
Soluble in DMSO
Description
Orally active dual FAK/PYK2 inhibitor (IC50 value 1.5 nM and ~100 nM in vitro and in vivo, respectively) that blocks FAK and p130Cas (130 kDa Crk-associated substrate) tyrosine phosphorylation, promotes caspase-3 activation, and selectively triggered cell apoptosis in tumor cells in 3D environments. PND1186 inhibitory effects differ from Dasatinib (Axon 1392; as it does not affect c-Src activity), and prevents spontaneous breast to lung metastasis in pre-clinical models. PND-1186 inhibits cell growth in multiple myeloma (MM) cells both in vitro and in vivo by inhibition of PYK2 (IC50 and EC50 values 85 nM and 20 nM, respectively).
References
Certificates
Categories
Extra info
I. Tanjoni et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.
C. Walsh et al. Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol Ther. 2010 May 15;9(10):778-90.
Y. Zhang et al. Pyk2 promotes tumor progression in multiple myeloma. Blood. 2014 Oct 23;124(17):2675-86.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
FAK
PYK2
Wnt-β-Catenin
MAPK
EC 2.7.10.2
Orally active dual FAK/PYK2 inhibitor triggering cell apoptosis in tumor cells
Chemical name
2-(2-(2-methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide
Parent CAS No.
[1061353-68-1]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |