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An orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Upon oral administration, ASK1 inhibitor GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. This prevents the phosphorylation of downstream kinases, such as c-Jun N-terminal kinases (JNKs) and p38 mitogen-activated protein kinase (p38 MAPK). By preventing the activation of ASK1-dependent signal transduction pathways, GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.
| Molecular Weight | 445.49 |
| Formula | C24H24FN7O |
| CAS Number | 1448428-04-3 |
| Solubility (25°C) | 36 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related p38 MAPK Products |
|---|
| BIRB796
BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK with Kd of 100pM. |
| Adezmapimod
Adezmapimod (SB203580) is a P38 MAPK inhibitor with an IC50 of 0.3-0.5 μM, which is 10 times less selective than SAPK3(106T) and SAPK4(106T), and inhibits PKB phosphorylation with an IC50 of 3-5 μM. |
| SB 202190
SB 202190 is a highly selective, potent and cell permeable inhibitor of p38 MAP kinase with IC50 values of 50 and 100 nM inhibiting p38α and p38β, respectively. |
| PH-797804
PH-797804 is a highly selective and potent inhibitor of p38 MAP kinase with IC50 of 26 nM. |
| VX-702
VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM. |
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Products are for research use only. Not for human use. We do not sell to patients.
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