Physical Appearance:  White solid

Molecular Formula:  C₂₁H₁₆FN₃OS

Molecular Weight:  377.4

Purity:  >99% (TLC)

Solubility:  Soluble in DMSO (50 mg/ml)

Storage:  Freezer (-20℃). Protect from light. Following reconstitution, aliquot and freeze (-20℃). This product is stable for 5 years as supplied. Stock solution are stable for up to 6 months at -20℃.

Description:  A highly specific, cell-permeable inhibitor of p38 kinase (IC₅₀=34nM in vitro, 600nM in cells). Inhibition is competibive with ATP (Ki=21nM). Inhibites p38 MAPK stimulation of MAPKAPK2 (IC₅₀=70nm). Also known as reactivating kinase (RK) and CSBP (cytokine synthesis anti-inflammatory drug binding protein). Does not significantly inhibit JNK or p42 MAP kinase even at 100μM Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC₅₀=50-100nM). SB 203580 has also been shown to be an effective inhibitor of inflammatory cytokine production in vivo in both mice and rats.

References:

1.      A.Cuenda et al. FEBS Lett. 1985 364 229

2.      P.R.Young et al. J.Biol.Chem. 1997 272 12116

3.      A.Clerk et al. FEBS Lett. 1998 426 93

4.      A.G.Borsch-Haubold et al. J. Biol. Chem. 1998 273 28766

The pharmacological and toxicological properties of this product have not been fully investigated.  Exercise caution in use and handling.  This product must not be used in humans.