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General description
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. 654205m and actinomycin D (1 g/mL; Cat. Nos. 114666) 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. 34539m) & 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
Cell permeable: yes
Primary Target
TNFα
Reversible: yes
Target Ki: 110 nM for hTNF&alpha
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Use only fresh DMSO for reconstitution.
Other Notes
Ma, L., et al. 2014. J. Biol. Chem.289, 12457.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Segment | 100 |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | dark red |
| solubility | DMSO: 5 mg/mL |
| storage temp. | 2-8°C |
| 长度(mm) | |
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| 重量(kg) |
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¥ 1573.49
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¥ 1779.22
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¥ 1451.54
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¥ 9207.92
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¥ 5014.59
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NALGENE 180透明塑料管，透明，柔软，多用，经济，内径 x 外径x壁厚，1/8 x 1/4 x 1/16，英寸，每箱数量50，50/箱，8000-0020，Thermofisher，赛默飞世尔询价
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