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CAS No.: 1473404-51-1

Hck-IN-1 Catalog No. CSN25623

Hck Blocker compound B9 is a Nef-dependent Hck blocker with IC50 value of 2.8μM for Nef-Hck complex but >20μM for Hck alone. It binds directly to Nef via a pocket formed by the Nef dimerization interface and disrupts Nef dimerization in cells.

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实验方案

技术信息

生物活性

描述Hck is a member of the Src-family that serves a key effector role in Nef-dependent human immunodeficiency virus (HIV)-1 replication. Hck-IN-1 is a selective Nef-dependent Hck inhibitor with IC50 values of 2.8μM and >20μM for the Nef:Hck complex and Hck alone, respectively, in vitro. In CEM-T4 cells, Hck-IN-1 inhibited wild-type HIV-1 replication with IC50 values of 100 – 300nM, while replication of Nef-defective HIV-1 was not affected at 3.0μM. Hck-IN-1 also inhibited the replication of all eleven HIV-1 Nef chimeras tested in CEM-T4 cell with an IC50 value of ~300nM. In HIV-infected cells, B9 completely inhibited Nef-dependent SFK activation at a concentration of 1.0μM. B9 inhibited the replication of simian immunodeficiency virus with an IC50 value of ~1.0 μM^[1].
参考文献

[1] Emert-Sedlak LA, Narute P, Shu ST, Poe JA, Shi H, Yanamala N, Alvarado JJ, Lazo JS, Yeh JI, Johnston PA, Smithgall TE. Effector kinase coupling enables high-throughput screens for direct HIV-1 Nef antagonists with antiretroviral activity. Chem Biol. 2013 Jan 24;20(1):82-91.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4825 mL
- 12.4126 mL
- 24.8253 mL
- 5 mM
- 0.4965 mL
- 2.4825 mL
- 4.9651 mL
- 10 mM
- 0.2483 mL
- 1.2413 mL
- 2.4825 mL

技术信息

CAS号

1473404-51-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H11ClN6O3S

运输

蓝冰

分子量

402.81

别名

溶解度

DMSO	12.0 mg/mL (29.8 mM) warming

动物实验配方

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