SB202190是一种有效的p38 MAPK抑制剂，靶向作用于p38α/β，无细胞试验中IC50为50 nM/100 nM，有时用于代替SB 203580研究其在体内对SAPK2a/p38的潜在作用。SB202190 可通过诱导自噬和血红素氧化酶1来抑制内皮细胞的凋亡。SB202190可显著抑制Erastin依赖的铁死亡ferroptosis。
| CAS No. | 152121-30-7 |
| 生物活性 | SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits. SB202190 induces autophagy. |
| 分子式 | C20H14FN3O |
| 分子量 | 331.34 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存条件 | Powder -20°C 3 years |
| 溶解性数据 | DMSO : 100 mg/mL (301.80 mM; Need ultrasonic) |
| 体内研究 | SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) shows inhibition of tumor cell survival and tumor growth. |
| 体外研究 | SB 202190 (0-10 μM; 0-72 hours) attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner. SB 202190 strongly inhibited colony formation and anchorage-independent growth (10 μM for 7–10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480). In RKO, CACO2 and SW480 cells, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling. |
| 纯度及产品资料 | 98% |
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