Nef Hck Activation Inhibitor, B9 (Nef Dimerization Blocker, (E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide)

Size

£479.00

SKU:: 217581
Molecular Weight:: 402.81
Purity:: ≥98% (HPLC)
Storage Conditions:: 4°C
Supplier:: United States Biological
CAS Number:: 1596216-24-8
Format:: Supplied as an orange powder.
Extra Details:: A cell-permeable diphenylpyrazolo compound that disrupts HIV accessary protein Nef dimerization (IC50 = 3uM in HEK293T cells) and prevents Nef-mediated Src family kinase Hck activation (IC50 = 2.8uM) without directly affecting the catalytic activity of c-Src, Hck, Lck, or Lyn. Shown to suppress HIV and SIV viral replication (IC50/strain/culture = 1uM/SIV deltaB670/CEM-174 and <0.3uM/HIV-1 NL4-3/CEM-T4) and infectivity, being ineffective against the replication of Nef-defective HIV-1 mutant. Molecular docking and in vitro binding studies reveal a high-affinity B9-targeting site formed at the Nef dimerization interface and a low-affinity binding site on each Nef monomer at the dimer interface periphery. CAS No: 1596216-24-8 Molecular Formula: C₁₆H₁₁ClN₆O₃S Primary Target: Nef Solubility: DMSO Storage and Stability: Store at 4°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.