Chemical Name:3-(Dimethylamino)-N-[3-[(4-hydroxybenzoyl)-amino]-4-met
hylphenyl]benzamide
Biological Activity:
Potent, selective inhibitor of c-Raf in vitro (IC50 =
70 nM for inhibition of human c-Raf). Shows 10-fold selectivity over B-Raf.
Also inhibits SAPK2/p38 (IC50 = 2 μM). Selective over 17 other protein kinases including PKA,
PKC, p42 MAPK, CDK1 and SAPK1/JNK (up to 50 μM).
Hall-Jacksonet al (1999) Paradoxical activation of Raf by a
novel Raf inhibitor. Chem.Biol. 6 559. Wartenberget al
(2001) Down-regulation of intrinsic p-glycoprotein expression in multicellular
prostate tumor spheroids by reactive oxygen species. J.Biol.Chem. 276
17420.