HPN-01 |
| カタログ番号GC63007 |
HPN-01 は強力かつ選択的な IKK 阻害剤であり、IKK-α、IKK-β、IKK-ε の pIC50 値はそれぞれ 6.4、7.0、<4.8 です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 928655-63-4
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[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.
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