SB 203580 (CAS No: 152121-47-6), #abs810002

Description

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3 (106T) and SAPK4 (106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.

Purity

99%

Stability & Storage

Store at -20℃ for one year (Powder);

In DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

Other names

RWJ 64809; PB 203580; SB203580; SB-203580

Appearance

Lyophilized powder

Solubility

DMSO: 43 mg/mL (113.92 mM)

Biological Activity

Target

p38 MAPK, PKB

In vitro

SB203580 inhibits 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 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells.

In vivo

SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE).

References

References

[1] Ferdinand V. Lali, et al. J Biol Chem, 2000, 275(10), 7395-402.

[2] Birkenkamp KU, et al. Br J Pharmacol, 2000, 131(1): 99-107.

[3] Zhang H, et al. Apoptosis, 2011