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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 |
|---|
| SSK1
SSK1 is a senescence-specific killing compound and is a precursor for β-galactosidase, which can reduce the inflammatory response. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in senescent cells, promote mitochondrial DNA damage and selectively killed senescent cells. |
| p38 MAP Kinase Inhibitor III
p38 MAP Kinase Inhibitor III is a p38 MAPK inhibitor with an IC50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with IC50 values of 0.37 μM and 0.044 μM, respectively. |
| (R)-STU104
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. |
| SB 706504
SB 706504 is a potent p38 MAPK inhibitor that inhibits Lipopolysaccharides-stimulated inflammatory gene expression in macrophages in chronic obstructive pulmonary disease (COPD). |
| RWJ-67657
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. |
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