HPN-01 是一种有效选择性的 IKK 抑制剂，对 IKK-α、IKK-β 和 IKK-ε 的 pIC₅₀ 6.4、7.0 和 <4.8。HPN-01 比 50 多种其他激酶显示出大于50倍的选择性，包括 ALK5、CDK-2、EGFR、ErbB2、GSK3β、PLK1、Src 和 VEGFR-2。

HPN-01 is a potent and selective IKK inhibitor, with pIC 50 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.

Solid

IKK-α 6.4 (pIC50) IKK-β 7.0 (pIC50

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).
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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 100 mg/mL (248.84 mM; Need ultrasonic)配制储备液