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500653 Nef Hck Activation Inhibitor, B9 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₁₁ClN₆O₃S

Products

Catalog NumberPackaging Qty/Pack
5.00653.0001 Glass bottle 10 mg
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
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
Catalog Number GTIN
5.00653.0001 04055977245042

Documentation

Nef Hck Activation Inhibitor, B9 - Calbiochem 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
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
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.