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In vitro: SKF-86002 inhibited prostaglandin H2 (PGH2) synthase activity (IC50 120 microM) as well as prostanoid production by rat basophilic leukemia (RBL-1) cells (IC50 70 microM) and its sonicate (IC50 100 microM) and human monocytes (IC50 1 microM). In addition, SK&F 86002 inhibited the generation of dihydroxyeicosatetraenoic acid (diHETE) and 5-hydroxyeicosatetraenoic acid (5-HETE) by a high speed supernatant fraction of RBL-1 cells (IC50 10 microM). differentiation of HL-60 cells toward the neutrophil phenotype resulted in a loss in c-Jun NH2-terminal kinase activation with concomitant acquisition of formylmethionylleucylphenylalanine-stimulatable and stress-inducible p38 MAPK activity as well as apoptosis blockade by SKF-86002. SKF-86002 blocked superoxide anion production in response to FMLP and reduced adhesion and chemotaxis in response to PAF or FMLP.
| Molecular Weight | 297.35 |
| Formula | C16H12FN3S |
| CAS Number | 72873-74-6 |
| Solubility (25°C) | 10 mM 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 |
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BIRB 796 (Doramapimod) is a protein kinase inhibitor of p38 MAPK with Kd of 100pM. |
| Selonsertib
GS-4997 is a highly selective and potent once-daily oral ASK1 inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. |
| 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. |
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