| Identification | Back Directory | [Name]
TC ASK 10 | [CAS]
1005775-56-3 | [Synonyms]
TC ASK 10
ASK1 Inhibitor 10
4-tert-butyl-N-(6-imidazol-1-ylimidazo[1,2-a]pyridin-2-yl)benzamide:hydrochloride
4-(1,1-Dimethylethyl)-N-[6-(1H-imidazol-1-yl)imidazo[1,2-a]pyridin-2-yl]benzamide dihydrochloride | [Molecular Formula]
C21H21N5O.2HCl | [MDL Number]
MFCD26792581 | [MOL File]
1005775-56-3.mol | [Molecular Weight]
395.89 |
| Chemical Properties | Back Directory | [Melting point ]
>270° (dec.) | [storage temp. ]
Refrigerator, under inert atmosphere | [solubility ]
DMSO (Slightly), Methanol (Slightly) | [form ]
Solid | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Description]
ASK1 inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1; IC50 = 14 nM). It is selective for ASK1 over ASK2 (IC50 = 510 nM) as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF (IC50s = >10,000 nM for all). It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner. | [Uses]
TC ASK 10 is a potent ASK1 inhibitor. It displays selectivity for ASK1 over other kinases including ASK2, MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf. It blocks downstream JNK1/p38 phosphorylation in cells. | [in vivo]
Pharmacokinetic profiles in rats are tested. TC ASK 10 (Compound 10 HCl; rat cassette doing at 0.1 mg/kg, iv and 1 mg/kg, po.) has a good oral bioavailability. The Cmax, Tmax and AUCpo,0-8h are 285.1 ng/mL, 1.67 h and 275.4 ng.h/mL, respectively for TC ASK 10[1]. | [IC 50]
ASK1: 14 nM (IC50) | [storage]
Desiccate at RT | [References]
[1] YOSHITO TERAO. Design and biological evaluation of imidazo[1,2-a]pyridines as novel and potent ASK1 inhibitors[J]. Bioorganic & Medicinal Chemistry Letters, 2012, 22 24: Pages 7326-7329. DOI: 10.1016/j.bmcl.2012.10.084 |
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| Company Name: |
BOC Sciences
|
| Tel: |
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| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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