Brief Description

Pyridone 6(CMP 6) is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
IC50 value: 15/1/5/1 nM (JAK1/JAK2/JAK3/Try2)
Target: pan JAK
Pyridone 6, a pan-JAK inhibitor, delayed the onset and reduced the magnitude of skin disease in an AD-like skin-disease model of NC/Nga mice. Pyridone 6 displays potent inhibitory activity against JAK1 (IC50 = 15 nM for murine JAK1), JAK2 (IC50 = 1 nM), JAK3 (Ki = 5 nM), and Tyk2 (IC50 = 1 nM). Pyridone 6 is therapeutic for AD by modulating the balance of Th2 and Th17. JAK inhibitor Pyridone 6 suppresses asthmatic responses by inhibiting Th2 inflammation and that application of PLGA nanoparticles improves the therapeutic potency of Pyridone 6.
Inhibition of JAK may be useful for the treatment of bone-resorptive diseases, such as osteoporosis. Pyridone 6 is a more sensitive and specific inhibitor of JAK-STAT3 activity compared with AG490 and potently inhibited the growth of primary myeloma cells and myeloma-derived cell lines grown on BMSCs.

Solubility

DMSO 5 mg/ml

Melting point

Boiling point

Density

Formula Weight:

Flash point

Storage conditions

Store at -20°C 2 years

Appearance:

Light brown to brown solid