Hck-IN-1 是二苯基吡唑啉化合物，选择性的 Nef 依赖性Hck抑制剂。它是广泛的HIV-1 Nef直接拮抗剂，对于野生型 HIV-1 复制的IC50为 100-300 nM。它结合口袋残基 Asn126，具有抗逆转录病毒活性。

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

Hck-IN-1 inhibits the replication of all eleven HIV-1 Nef chimeras (IC50s: ~ 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.?Hck-IN-1 ?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.

1473404-51-1

C16H11ClN6O3S

402.82

DMSO:12.5 mg/mL (31.03 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years