Physical Appearance:  Pale yellow solid

Molecular Formula:  C₂₀H₁₄FN₃O

Molecular Weight:  331.3

Purity:  99% (TLC)

Solubility:  DMSO (50mg/ml)

Storage:  FREEZER (-20℃). Protect from light. Following reconstitution, aliquot and freeze (-20℃). This product is stable for 3 years as supplied. Stock solutions are stable for up to 6 months at -20℃.

Description:  A potent and cell-permeable inhibitor of p38 MAP kinase (IC₅₀=30nM). Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgrounds. Also inhibits the kinase activity of p38β (IC₅₀=16nM in vitro and 350nM in cells) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC₅₀=280nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells.

References:

1.      J.C.Lee et al. Nature 1994 372 739

2.      Z.A.Cuenda et al. FEBS Lett. 1995 364 229

3.      T.Fox et al. Protein Sci. 1998 7 2249

4.      R.P.Singh et al. J.Biol.Chem. 1999 274 19593

5.      S.Nemoto J.Biol.Chem. 1998 273 16415

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.