4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol

JAK3 inhibitor, IC50 = 78 µM

OTAVAchemicals Catalogue Number: 7015070103

CAS Registry Number: 202475-60-3

Purity: 97% (HPLC)

Ref.: Clin. Canc. Res. 1999, 5, 1569 - 1582 J. Biol. Chem. 1999, 274, 38, 27028 - 27038  Cellular & Molecular Immunology 2012, 9, 350, 360 Int. J. Mol. Med. 2012, 29, 864 , 870

Abstract: WHI-P131 showed potent JAK3-inhibitory activity. WHI-P131 inhibited the clonogenic growth of JAK3-positive leukemia cell lines DAUDI, RAMOS, LC1;19, NALM-6, MOLT-3, and HL-60. Selective inhibition of JAK3 in mast cells with WHI-P131 blocked the phospholipase C activation, calcium mobilization, and activation of microtubule-associated protein kinase after lgE receptor/FceRI cross-linking. JAK3 inhibition by WHI-P131 promotes TGF-secretion by CD4+ T cells in vitro and in vivo.

Induction of these cells might be the underlying mechanism of antidiabetogenic action of WHI-P131 in NOD mice. Inhibition of the JAK/STAT pathway by JANEX-1 ameliorates the TNF-alpha-induced cell adhesion molecule expression in endothelial cells and may modulate the vascular inflammatory process in sepsis.

DOI: 

10.1074/jbc.274.38.27028

10.1038/cmi.2012.20

10.3892/ijmm.2012.920