Hck-IN-1 (compound B9) 是一种二苯基吡唑啉化合物，选择性的 Nef 依赖性 Hck 抑制剂，对 Nef：Hck 复合物和 Hck 的 IC₅₀ 分别为 2.8 μM 和 >20 μM。Hck-IN-1 是一种直接且广泛的 HIV-1 Nef 拮抗剂，对于野生型 HIV-1 复制的 IC₅₀ 为 100-300 nM。Hck-IN-1 结合口袋残基 Asn126，具有抗逆转录病毒活性。

Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC 50 s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC 50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity.

Solid

HIV-1 Nef 100-300 nM (IC50)

Hck-IN-1 (compound B9) shows weak activity against other Src-family members in vitro, with IC50 values >20 μM for c-Src, Lck and Lyn.
B9 (1 μM; 8 days) completely inhibits Nef-dependent SFK activation at a concentration of 1.0 μM.
Hck-IN-1 (0.1, 0.3, 1, 3 μM) also inhibits Nef-mediated enhancement of HIV-1 infectivity in a concentration-dependent manner in the reporter cell line, TZM-bl.
Hck-IN-1 inhibits the replication of all eleven HIV-1 Nef chimeras with IC50 values of ~ 300 nM in CEM-T4 cells, demonstrating that the compound is broadly active against HIV replication supported by a wide range of HIV-1 Nef proteins.
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]. Emert-Sedlak LA, et al. 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.

In Vitro: DMSO : 12.5 mg/mL (31.03 mM; Need ultrasonic)配制储备液