HPN-01

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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.

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).

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Immunology/Inflammation

IκB kinase (IKK)

IκB/IKK

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928655-63-4

401.87

C19H16ClN3O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (248.84 mM; 超声助溶 )

NC(=O)c1cc(cc(c1N)-c1ccc(cc1)S(N)(=O)=O)-c1ccc(Cl)cc1

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(-20℃)

With Ice Pack

≥ 2 years