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ASK1-IN-2

Catalog No. T9377   CAS 2541792-70-3

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can potentially be used as a therapeutic strategy for ulcerative colitis[1].

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ASK1-IN-2 Chemical Structure
ASK1-IN-2, CAS 2541792-70-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 87.00
5 mg In stock $ 213.00
10 mg In stock $ 343.00
25 mg In stock $ 583.00
50 mg In stock $ 835.00
100 mg In stock $ 1,150.00
500 mg In stock $ 2,290.00
1 mL * 10 mM (in DMSO) In stock $ 235.00
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Purity: 99.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can potentially be used as a therapeutic strategy 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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 249 mg/mL (683.35 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Hou S, et, al. Structure-based discovery of 1H-indole-2-carboxamide derivatives as potent ASK1 inhibitors for potential treatment of ulcerative colitis. Eur J Med Chem. 2020 Dec 24;211:113114.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Inhibitor Library Cytoskeletal Signaling Pathway Compound Library Anti-Obesity Compound Library Anti-Colorectal Cancer Compound Library Bioactive Compounds Library Max Orally Active Compound Library Reprogramming Compound Library Anti-Prostate Cancer Compound Library NO PAINS Compound Library

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Keywords

ASK1-IN-2 2541792-70-3 Apoptosis MAPK ASK colitis ulcerative signal-regulating ASK1 IN 2 ASK1IN2 inhibit MAP kinase kinase kinase, MEKK, MAPKKK ASK1 Inhibitor ASK-1-IN-2 MAP3K inhibitor

 

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