JAK3 INHIBITOR I

Description

WHI-P131 (202475-60-3) is a JAK3 inhibitor.?Inhibits human glioblastoma cell adhesion and invasion.1 Increases survival in a mouse ALS model.2 Delays or prevents autoimmune type 1 diabetes in NOD mice.3 Exhibits potent anti-inflammatory activity in mouse models of peritonitis, colitis, cellulitis and systemic inflammatory response syndrome.4 Displays protective effects against myocardial ischemia and reperfusion injury in mouse models.5

The Uses of JAK3 INHIBITOR I

Janex 1 is a Janus tyrosine kinase 3 (JAK3) inhibitor. Inhibition of JAK3 has been shown to exhibit protective action against the development of T1D in non-obese diabetic (NOD) mice. Janex 1 has been shown to suppresses proliferation of short-term cultured NOD CD4+ T cells through induction of apoptosis, while promoting survival of a particular population of long-term cultured cells. It ameliorates the expression of TNF-α-induced cell adhesion molecules and improves myocardial vascular permeability.

What are the applications of Application

Janex-1 is a selective inhibitor of tyrosine kinase activity of JAK3

References

1) Narla et al. (1998), Inhibition of human glioblastoma cell adhesion and invasion by 4-(4’-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P131) and 4-(3’-bromo-4’-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P154); Mol. Clin. Cancer Res., 4 2463 2) Trieu et al. (2000), A specific inhibitor of janus kinase-3 increases survival in a transgenic mouse model of amyotrophic lateral sclerosis; Biochem. Biophys. Res. Commun., 267 22 3) Cetkovic-Cvrlje et al. (2003), Targeting JAK3 with JANEX-1 for prevention of autoimmune type 1 diabetes in NOD mice; Clin. Immunol., 106 213 4) Uckun et al. (2008), Anti-inflammatory activity profile of JANEX-1 in preclinical animal models; Bioorg. Med. Chem., 16 1287 5) Oh et al. (2013), Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice; Exp. Mol. Med., 45 e23