您的位置：首页 > 产品中心 > TNF-TNFR Interaction Modulator, C87-Calbiochem
TNF-TNFR Interaction Modulator, C87-Calbiochem
| 产品编号： | 4083750 |
| 规格： | Inhibits TNFα/β-stimulated biological activity by modulating, but not abolishing, TNF-TNFR interaction via direct TNF affinity interaction (KD = 110 nM). |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
TNF-TNFR Interaction Modulator, C87-Calbiochem
( 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
基本信息
| Empirical Formula【经验(实验)分子式】 | C24H15ClN6O3S |
| Molecular weight | 502.93 |
| General description【一般描述】 | 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 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 g/mL; Cat. Nos. 114666 & 2472-OP) treatment (EC50 = 8.73 M 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 g/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. |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Target Ki: 110 nM for hTNF&alpha Primary Target TNFα Reversible: yes |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Use only fresh DMSO for reconstitution. Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. |
| Other Notes【其他说明】 | Ma, L., et al. 2014. J. Biol. Chem.289, 12457. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥97% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | dark red |
| solubility【溶解性】 | DMSO: 5 mg/mL |
| storage temp.【储存温度】 | 2-8℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
