1. NF-κB
  2. IKK
  3. HPN-01

HPN-01 

目录号: HY-135366
产品使用指南

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。

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HPN-01 Chemical Structure

HPN-01 Chemical Structure

CAS No. : 928655-63-4

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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].

IC50 & Target[1]

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].

Molecular Weight

401.87

Formula

C₁₉H₁₆ClN₃O₃S

CAS No.

928655-63-4

SMILES

O=C(C1=C(N)C(C2=CC=C(S(=O)(N)=O)C=C2)=CC(C3=CC=C(Cl)C=C3)=C1)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

HPN-01HPN01HPN 01IKKIκB kinaseI kappa B kinaseLPSsecretionPBMCNF-κBnucleartranslocationNAFLDInhibitorinhibitorinhibit

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产品名称:
HPN-01
目录号:
HY-135366
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