SB 203580

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种特异性p38 MAPK抑制剂，IC50为0.6 uM；显示出对 JNK、p42 MAPK、p90 S6K、p70 S6K、PKA 等的选择性。

A specific p38 MAPK inhibitor with IC50 of 0.6 uM; shows selectivity over JNK, p42 MAPK, p90 S6K, p70 S6K, PKA, etc.; suppresses the activation of MAPKAP kinase-2 and prevents the phosphorylation of HSP27 in response to interleukin-1, cellular stresses and bacterial endotoxin in vivo.(In Vitro):Adezmapimod (SB 203580) (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.SB203580 blocks PKB phosphorylation (IC50 3-5 μM). SB203580 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.(In Vivo):Adezmapimod (SB 203580) (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.

Cell Proliferation Assay Cell Line:CT6, BA/F3 cell line F7, and PBMC/T cells Concentration:0-30 μMIncubation Time:Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2Result:Prevented 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. Western Blot Analysis Cell Line:CT6 cells, activated human T cells, and BA/F3 F7 cells Concentration:0-30 μM Incubation Time:Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min Result:Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner.

Animal Model:Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors Dosage:5 mg/kg/day Administration:Intra peritoneal injected daily for 16 consecutive days Result:After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10).

RWJ 64809 | SB203580 | SB-203580

MAPK/ERK Signaling

p38 MAPK

p38MAPK

Cancer

——

152121-47-6

377.4346

C21H16FN3OS

>98% (HPLC)

DMSO: ≥ 33 mg/mL

O=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C

Pyridine, 4-[4-(4-fluorophenyl)-2-[4-(methylsulfinyl)phenyl]-1H-imidazol-5-yl]-

(-20℃)

With Ice Pack

≥ 2 years