500653 | Nef Hck Activation Inhibitor, B9 - Calbiochem

500653
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₆H₁₁ClN₆O₃S

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.00653.0001
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          Glass bottle 10 mg
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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®
          SynonymsNef Dimerization Blocker, (E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide
          References
          ReferencesEmert-Sedlak, L.A., et al. 2013. Chem. Biol. 20, 82.
          Product Information
          FormOrange powder
          Hill FormulaC₁₆H₁₁ClN₆O₃S
          Chemical formulaC₁₆H₁₁ClN₆O₃S
          ReversibleY
          Structure formula ImageStructure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Emert-Sedlak, L.A., et al. 2013. Chem. Biol. 20, 82.
          Data Sheet

          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
          SynonymsNef Dimerization Blocker, (E)-4-((3-Chlorophenyl)diazenyl)-5-hydroxy-3-(4-nitrophenyl)-1H-pyrazole-1-carbothioamide
          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
          Chemical formulaC₁₆H₁₁ClN₆O₃S
          Structure formulaStructure formula
          Purity≥98% by HPLC
          SolubilityDMSO (2.5 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesEmert-Sedlak, L.A., et al. 2013. Chem. Biol. 20, 82.