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530796 TNF-TNFR Interaction Modulator, C87 - CAS 332420-90-3 - Calbiochem

Inhibits TNFα/β-stimulated biological activity by modulating, but not abolishing, TNF-TNFR interaction via direct TNF affinity interaction (KD = 110 nM).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: (E)-4-(2-(4-Chloro-3-nitrophenyl)hydrazono)-3-phenyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one, (E)-4-(2-(4-Chloro-3-nitrophenyl)), TNF-TNFR Signaling Inhibitor IV

Primary Target: TNFα
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530796
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Overview

Key Spec Table

CAS #Empirical Formula
332420-90-3C₂₄H₁₅ClN₆O₃S

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      		 Glass bottle 10 mg
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      Description
      OverviewA phenylhydrazonodihydropyrazolone compound that inhibits TNFα/β-stimulated biological activity by modulating, but not abolishing, TNF-TNFR interaction via direct TNF affinity interaction (KD = 110 nM). Shown to prevent murine L929 cell death following hTNFα/β (1 ng/mL; Cat. Nos. 654205 & 654215) and actinomycin D (1 µg/mL; Cat. Nos. 114666 & 2472-OP) treatment (EC50 = 8.73 µM) by blocking TNF/ActD-induced caspase-3/8 cleavages & IκBα degradation without affecting Fas- (CD95) mediated Jurkat cell death or VP-16 (Etoposide; Cat. No. 341205) and ADR (Adriamycin/Doxorubicin; Cat. No. 324380) cytotoxicity in L292 cultures. When applied prior to D-galactosamine (1.2 g D-GalN/kg, Cat. No. 34539) & Lipopolysaccharide (LPS; 50 µg/kg) injection, C87 effectively prevents D-GalN/LPS-induced upregulation of plasma alanine transaminase & aspartate transaminase (ALT & AST) activity, resulting in significantly reduced liver damage and much improved survival rate (3X 12.5 mg C87/kg i.p. dosings 16, 8, & 1 h prior to D-GalN/LPS injection) in a murine hepatitis model in vivo.
      Catalogue Number530796
      Brand Family Calbiochem®
      Synonyms(E)-4-(2-(4-Chloro-3-nitrophenyl)hydrazono)-3-phenyl-1-(4-phenylthiazol-2-yl)-1H-pyrazol-5(4H)-one, (E)-4-(2-(4-Chloro-3-nitrophenyl)), TNF-TNFR Signaling Inhibitor IV
      References
      ReferencesMa, L., et al. 2014. J. Biol. Chem. 289, 12457.
      Product Information
      CAS number332420-90-3
      FormDark red solid
      Hill FormulaC₂₄H₁₅ClN₆O₃S
      Chemical formulaC₂₄H₁₅ClN₆O₃S
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetTNFα
      Primary Target K<sub>i</sub>110 nM for hTNF&alpha
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      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
      Global Trade Item Number
      Catalogue Number GTIN
      5.30796.0001 04055977242973