详情描述
SB203850 is a p38 MAPK inhibitor. SB203580 inhibits the phosphorylation of heat shock protein (HSP) 27 in response to IL-1, cellular stresses and bacterial endotoxin in vivo. SB203850 is useful for studying the physiological roles and targets of p38 MAPK and MAPKAP kinase-2.
Product information
CAS Number: 152121-47-6
Molecular Weight: 377.43
Formula: C21H16FN3OS
Synonym:
Adezmapimod
SB203850
SB-203850
Chemical Name: 4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)-1H-imidazole
Smiles: CS(=O)C1C=CC(=CC=1)C1NC(=C(N=1)C1C=CC(F)=CC=1)C1C=CN=CC=1
InChiKey: CDMGBJANTYXAIV-UHFFFAOYSA-N
InChi: InChI=1S/C21H16FN3OS/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15/h2-13H,1H3,(H,24,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 43 mg/mL(113.92 mM). Water: Insoluble.
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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:
- Zhang H, et al. Apoptosis, 2011
- Birkenkamp KU, et al. Br J Pharmacol, 2000, 131(1): 99-107.
- Ferdinand V. Lali, et al. J Biol Chem, 2000, 275(10), 7395-402.
Products are for research use only. Not for human use.