Pyridone 6

Pyridone 6

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Pyridone 6 (457081-03-7) is a 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

References:

  1. Thompson et al. (2002) Photochemical preparation of a pyridine containing tetracycle: a JAK protein kinase inhibitor Med. Chem. Lett. 12 1219
  2. Mae et al. (2010) Combination of small molecules enhances differentiation of mouse embryonic stem cells into intermediate mesoderm through BMP7-positive cells; Biochem. Biophys. Res. Commun. 393 877
  3. Nakagawa et al. (2011) Pyridone 6, a pan-JAK inhibitor, ameliorates allergic skin inflammation of NC/Nga mice via suppression of Th2 and enhancement of Th17; Immunol. 187 4611
  4. Moriwaki et al. (2011) IL-13 suppresses double-stranded RNA-induced IFN-l production in lung cells; Biochem. Biophys. Res. Commun. 404 922
CAS:
457081-03-7

Catalog Number:
10-5555

Activity:
pan-JAK inhibitor

Chemical Names:
2-(tert-Butyl)-9-fluoro-1Hbenzo[h]imidazo[4,5-f]isoquinolin-7(6H)-one; JAK Inhibitor I

Molecular Weight:
309.34

Molecular Formula:
C18H16FN3O

Solubility:
Soluble in DMSO (30 mg/ml)

Physical Properties:
Off-white solid

Purity:
>98% HPLC
NMR (Conforms)

Storage Temperature:
-20°C

Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Shipping Code:
RT