Chemical Name: 2-(tert-Butyl)-9-fluoro-1Hbenzo[h]imidazo[4,5-f]isoquinolin-7(6H)-one. Alternate Names: JAK Inhibitor I
pan-JAK inhibitor
Molecular Weight:
309.34
Purity:
98% by HPLC NMR (Conforms)
Form:
Off-white solid
CAS Number:
[457081-03-7]
Formula:
C18H16FN3O
Application Notes:
Potent, ATP-competitive pan-JAK inhibitor. Inhibits 1, 2 and 3 (IC50=1, 5 and 15 nM respectively) as well as JAK family member Tyk2 (IC50=1 nM).1 Also tested against 21 other kinases with inhibition ranging from 130 nm to >10 mM. Inhibits IL2 and IL4-dependent proliferation of CTLL cells.1 Induces intermediate mesoderm differentiation from embryonic stem cells in a cocktail with LY-294002, CCG-1423 and retinoic acid.2 Potently inhibits STAT1, STAT5 and STAT6 phosphorylation and ameliorates allergic skin inflammation in a mouse model.3 Suppresses asthmatic responses in a mouse allergic asthma model.4
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