JAK3 INHIBITOR I Chemical Properties

Boiling point:

468.1±40.0 °C(Predicted)

Density 

1.336±0.06 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,2-8°C

solubility 

DMSO: 18 mg/mL, soluble

form 

solid

pka

10.06±0.26(Predicted)

color 

yellow

Stability:

Stable for 2 years from date of purchase as supplied. Protect from moisture. Solutions in DMSO may be stored at -20°C for up to 2 months.

Safety Information

Hazard Codes 

Xi

Risk Statements 

36/37/38

Safety Statements 

26-36

WGK Germany 

3

JAK3 INHIBITOR I Usage And Synthesis

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

Uses

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.

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

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