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SB 203580

SKU: orb1226156

Description

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.

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Key Properties

CAS Number152121-47-6
MW377.4346
Purity>98% (HPLC)
FormulaC21H16FN3OS
SMILESO=S(C1=CC=C(C2=NC(C3=CC=C(F)C=C3)=C(C4=CC=NC=C4)N2)C=C1)C
Targetp38 MAPK
SolubilityDMSO: ≥ 33 mg/mL

Bioactivity

In Vivo
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).
In Vitro
Cell Proliferation Assay Cell line: CT6, BA/F3 cell line F7, and PBMC/T cells. Concentration: 0-30 μM. Incubation time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2. Result: 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.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

RWJ 64809 | SB203580 | SB-203580

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SB 203580 (orb1226156)

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