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217581 Nef Hck Activation Inhibitor, B9 (Nef Dimerization Blocker, (E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide) CAS:

Specifications
Grade
Highly Purified
EU Commodity Code
38220090
Shipping Temp
Blue Ice
Storage Temp
4°C

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.

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.
Purity
≥98% (HPLC)
Form
Supplied as an orange powder.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
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