CAS No. : 869185-85-3
(Synonyms: SB 203580 (hydrochloride); RWJ 64809 (hydrochloride))
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10mg | $66 | In-stock |
50mg | $106 | In-stock |
100mg | $158 | In-stock |
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Cat. No. : | HY-10256A |
M.Wt: | 413.90 |
Formula: | C21H17ClFN3OS |
Purity: | >98 % |
Solubility: | H2O : 8.43 mg/mL (20.37 mM; Need ultrasonic and warming); DMSO : 100 mg/mL (241.60 mM; Need ultrasonic) |
Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator[1].
In Vitro: Adezmapimod hydrochloride (preincubated with 0-30 μM for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2) prevents the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM[1].
Adezmapimod hydrochloride blocks PKB phosphorylation (IC50 3-5 μM). Adezmapimod hydrochloride inhibitsthe phosphorylation of Ser473 in a dose-dependent manner in both CT6 and activated human T cells and IL-2-responsive BA/F3 F7 B cells[1].
In Vivo: Adezmapimod hydrochloride (5 mg/kg/day; intra peritoneal injected daily for 16 consecutive days, in female atymic Nu/Nu mice) treatment, p38WT tumors show a significantly smaller tumor burden when compared with p38TM tumors that were treated in parallel[1].
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