HPN-01
Names
[ CAS No. ]:
928655-63-4
[ Name ]:
HPN-01
Biological Activity
[Description]:
HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2[1].
[Related Catalog]:
[Target]
IKK-α:6.4 (pIC50)
IKK-β:7.0 (pIC50)
IKK-ε:<4.8 (pIC50)
[In Vitro]
HPN-01 effectively suppress LPS-stimulated secretion of TNF-α, IL-1β, and IL-6 from human PBMCs (pIC50=6.1, 6.4, and 5.7, respectively). HPN-01 also inhibits TNF-α-induced NF-κB nuclear translocation in human lung fibroblast cells (pIC50=5.7)[1]. HPN-01 inhibits the expression of SREBP-1and SREBP-2 in cultured primary human hepatocytes with IC50s of 1.71 μΜ and 3.43 μΜ, respectively. HPN-01 is being development for the treatment of nonalcoholic fatty liver disease (NAFLD)[2].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C19H16ClN3O3S
[ Molecular Weight ]:
401.87