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500653 Nef Hck Activation Inhibitor, B9 - CAS 1596216-24-8 - Calbiochem

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Synonymes: (E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide, Nef Dimerization Blocker

Primary Target: Nef
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500653
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Tableau de caractéristiques principal

CAS #Empirical Formula
1596216-24-8C₁₆H₁₁ClN₆O₃S

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      Description
      OverviewA cell-permeable diphenylpyrazolo compound that disrupts HIV accessary protein Nef dimerization (IC50 = 3 µM in HEK293T cells) and prevents Nef-mediated Src family kinase Hck activation (IC50 = 2.8 µM) without directly affecting the catalytic activity of c-Src, Hck, Lck, or Lyn. Shown to suppress HIV and SIV viral replication (IC50/strain/culture = 1 µM/SIV ΔB670/CEM-174 and <0.3 µM/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.
      Catalogue Number500653
      Brand Family Calbiochem®
      Synonyms(E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide, Nef Dimerization Blocker
      References
      ReferencesEmert-Sedlak, L.A., et al. 2013. Chem. Biol. 20, 82.
      Product Information
      CAS number1596216-24-8
      FormOrange powder
      Hill FormulaC₁₆H₁₁ClN₆O₃S
      Chemical formulaC₁₆H₁₁ClN₆O₃S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetNef
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5.00653.0001 04055977245042

      Documentation

      Nef Hck Activation Inhibitor, B9 - CAS 1596216-24-8 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Emert-Sedlak, L.A., et al. 2013. Chem. Biol. 20, 82.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision01-July-2013 JSW
      Synonyms(E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide, Nef Dimerization Blocker
      DescriptionA 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 (IC50 <0.3 µM in 9 d HIV-1 NL4-3-infected CEM-T4 cultures; IC50 = 1 µM in 5 d SIV ΔB670-infected CEM-174 cultures) and infectivity (45% and 50% inhibition against HIV-1 NL4-3 and SIV ΔB670, respectively, following 48 h 3 µM B9 treatment in TZM-bl reporter cells) in a Nef-dependent manner, being ineffective against the replication of Nef-defective HIV-1 mutant. Molecular docking studies predict a high-affinity B9-targeting site formed at the Nef dimerization interface and a low-affinity B9-binding site on each Nef monomer at the dimer interface periphery, with Asn126 contributing to both modes of binding. Consistently, in 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.
      FormOrange powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1596216-24-8
      Chemical formulaC₁₆H₁₁ClN₆O₃S
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (2.5 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesEmert-Sedlak, L.A., et al. 2013. Chem. Biol. 20, 82.