Hck-IN-1

SKU: orb1309586

Description

Hck-IN-1 is a selective small molecule antagonist of the HIV-1 Nef protein, potently inhibiting the Nef:Hck interaction and wild-type HIV-1 replication in vitro. It serves as a valuable chemical probe for studying Nef-dependent signaling in host cells and viral pathogenesis, with applications in retrovirology and antiretroviral drug discovery research.

Research Area

Cardiovascular Research, Infectious Disease & Virology, Protein Biochemistry, Signal Transduction

Key Properties

• CAS Number: 1473404-51-1
• MW: 402.81
• Purity: 99.07% (May vary between batches)
• Formula: C₁₆H₁₁ClN₆O₃S
• SMILES: NC(=S)n1nc(c(\N=N\c2cccc(Cl)c2)c1O)-c1ccc(cc1)[N+]([O-])=O
• Target: Src,HIV Protease,Hck
• Solubility: DMSO:12.5 mg/mL (31.03 mM)

Bioactivity

• Target IC50:
  HIV-1 (Nef):100-300 nM
• In Vitro:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

anti-retroviral, Asn126, diphenylpyrazolo, Human immunodeficiency virus, HIV, HIV Protease, HIV-1 Nef, HIVProtease, Hck, Hck IN 1, HckIN1, Hck-IN-1, Inhibitor, inhibit, Nef, Nef:Hck, Nef-dependent, Src, replication

Compound Identifiers

PubChem CID

4553981