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ASK1-IN-2 is a potent, orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. It has potential therapeutic applications for ulcerative colitis[1].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $68 | In Stock | |
5 mg | $163 | In Stock | |
10 mg | $263 | In Stock | |
25 mg | $476 | In Stock | |
50 mg | $715 | In Stock | |
100 mg | $1,070 | In Stock | |
1 mL x 10 mM (in DMSO) | $179 | In Stock |
Description | ASK1-IN-2 is a potent, orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. It has potential therapeutic applications for ulcerative colitis[1]. |
Targets&IC50 | ASK1:32.8 nM (IC50) |
In vitro | ASK1-IN-2 displays potent anti-ASK1 kinase activity and strong inhibitory effect on ASK1 in AP1-HEK293 cells with inhibition rate of 95.59%[1]. |
In vivo | ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T1/2=1.45 h) in rats[1]. ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUClast=4517 h?ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T1/2=2.31 h) in rats[1]. ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice[1]. ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues[1]. |
Molecular Weight | 364.38 |
Formula | C19H17FN6O |
Cas No. | 2541792-70-3 |
Smiles | CC(C)n1cnnc1-c1cccc(NC(=O)c2cc3ccc(F)cc3[nH]2)n1 |
Relative Density. | 1.41 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 249 mg/mL (683.35 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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