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MilliporeSigma™ Calbiochem™ Nef Hck Activation Inhibitor, B9
A cell-permeable diphenylpyrazolo compound that disrupts HIV accessary protein Nef dimerization (IC50 = 3μM in HEK293T cells) and prevents Nef-mediated Src family kinase Hck activation (IC50 )
Supplier: MilliporeSigma™ 5.00653.0001
Description
A cell-permeable diphenylpyrazolo compound that disrupts HIV accessary protein Nef dimerization (IC50 = 3μM in HEK293T cells) and prevents Nef-mediated Src family kinase Hck activation (IC50 = 2.8μM) without directly affecting the catalytic activity of c-Src, Hck, Lck, or Lyn. Shown to suppress HIV and SIV viral replication (IC50/strain/culture = 1μM/SIV δB670/CEM-174 and <0.3μM/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.Specifications
| Powder | |
| 10 mg | |
| 98% by HPLC | |
| C16H11ClN6O3S |
| Protect from light | |
| Orange | |
| Nef | |
| DMSO |
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