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928655-63-4

928655-63-4 structure
928655-63-4 structure
  • Name: HPN-01
  • Chemical Name: HPN-01
  • CAS Number: 928655-63-4
  • Molecular Formula: C19H16ClN3O3S
  • Molecular Weight: 401.87
  • Catalog: Signaling Pathways NF-κB IKK
  • Create Date: 2020-01-23 20:20:51
  • Modify Date: 2024-01-11 23:38:28
  • 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].

Name HPN-01
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

[1]. Christopher JA, et al. The discovery of 2-amino-3,5-diarylbenzamide inhibitors of IKK-alpha and IKK-beta kinases. Bioorg Med Chem Lett. 2007 Jul 15;17(14):3972-7.

[2]. Ke Li, et al. Amino-aryl-benzamide compounds and methods of use thereof.WO2018204775A1.

Molecular Formula C19H16ClN3O3S
Molecular Weight 401.87