Hck-IN-1


CAS No. : 1473404-51-1

1473404-51-1
Price and Availability of CAS No. : 1473404-51-1
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5mg $280 In-stock
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Cat. No. : HY-125028
M.Wt: 402.81
Formula: C16H11ClN6O3S
Purity: >98 %
Solubility: DMSO : 12.5 mg/mL (ultrasonic)
Introduction of 1473404-51-1 :

Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s 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 IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity[1]. IC50 & Target: IC50: 2.8 μM (Nef:Hck complex), >20 μM (Hck) and 100-300 nM (HIV-1 Nef)[1] In Vitro: 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[1].
B9 (1 μM; 8 days) completely inhibits Nef-dependent SFK activation at a concentration of 1.0 μM[1].
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[1].
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[1].

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