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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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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
332420-90-3C₂₄H₁₅ClN₆O₃S

Products

Catalog NumberPackaging Qty/Pack
5.30796.0001 Glass bottle 10 mg
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
Applications
Biological Information
Primary TargetTNFα
Primary Target K<sub>i</sub>110 nM for hTNF&alpha
Purity≥97% 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
5.30796.0001 04055977242973

Documentation

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

Title

Safety Data Sheet (SDS) 

References

Reference overview
Ma, L., et al. 2014. J. Biol. Chem. 289, 12457.
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.

Revision19-August-2014 JSW
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
DescriptionA 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 in binding study using hTNFα). 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 MTT assay; 20 h TNF/ActD treatment) 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 (58.5% vs. 20.8% with or without 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. A slow and long-lasting (>12 h) JNK T183/Y185 phosphorylation is induced upon TNFα stimulation in L929 cultures, while a much faster and more transient, albeit robust, TNFα-induced JNK pT183/Y185 is seen in the presence of C87 or a TNFα neutralizing antibody.
FormDark red solid
Intert gas (Yes/No) Packaged under inert gas
CAS number332420-90-3
Chemical formulaC₂₄H₁₅ClN₆O₃S
Purity≥97% by HPLC
SolubilityDMSO (5 mg/ml). Use only fresh DMSO for reconstitution.
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
ReferencesMa, L., et al. 2014. J. Biol. Chem. 289, 12457.