530796 Sigma-AldrichTNF-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).
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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
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Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 332420-90-3 | C₂₄H₁₅ClN₆O₃S |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 5.30796.0001 | Sklená flaša | 10 mg |
| Description | |
|---|---|
| Overview | A 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 Number | 530796 |
| 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 | |
|---|---|
| References | Ma, L., et al. 2014. J. Biol. Chem. 289, 12457. |
| Product Information | |
|---|---|
| CAS number | 332420-90-3 |
| Form | Dark red solid |
| Hill Formula | C₂₄H₁₅ClN₆O₃S |
| Chemical formula | C₂₄H₁₅ClN₆O₃S |
| Reversible | Y |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Primary Target | TNFα |
| Primary Target K<sub>i</sub> | 110 nM for hTNF&alpha |
| Purity | ≥97% by HPLC |
| Physicochemical Information | |
|---|---|
| Cell permeable | Y |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 5.30796.0001 | 04055977242973 |