Merck, 5006530001, Nef Hck Activation Inhibitor, B9

General description
A cell-permeable diphenylpyrazolo compound that is shown to disrupt HIV accessary protein Nef dimerization (IC₅₀ = 3 µM in HEK293T cells) and prevent Nef-mediated Src family kinase (SFK) Hck activation (IC₅₀ = 2.8 µM) without directly affecting the catalytic activity of c-Src, Hck, Lck, or Lyn (IC₅₀ >20 µM). Shown to effectively suppress HIV and SIV viral replication (IC₅₀in vitro binding studies reveal two B9 KD values of 1.72 nM and 860 nM toward full-length HIV-1 Nef and a complete loss of B9 binding toward Nef N126A/L/Q mutants.
Biochem/physiol Actions
Reversible: yes
Cell permeable: yes
Primary Target
Nef
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Emert-Sedlak, L.A., et al. 2013. Chem. Biol.20, 82.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)