| Bioactivity | C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM. | ||||||||||||
| Target | IC50: 8.73 μM (TNFα-induced cytotoxicity) | ||||||||||||
| Invitro | C 87 (C87) directly binds to TNFα, potently inhibits TNFα-induced cytotoxicity (IC50=8.73 μM) and effectively blocks TNFα-triggered signaling activities. C 87 exhibits good solubility and consistent dose-dependent functions in vitro. C 87 completely blocks TNFα-induced activation of caspase-3 and caspase-8. The activity of c-Jun N-terminal kinase (JNK) is significantly reduced by C 87 in L929 cells. C 87 also prevents the degradation of IκBα in cells treated with TNFα. C 87 potently blocks multiple signaling transduction pathways and downstream target gene activation triggered by TNFα[1]. | ||||||||||||
| In Vivo | C 87 (C87) attenuates TNFα-induced inflammation, thereby markedly reducing injuries to the liver and improving animal survival. C 87 injection delays the incidence of death and increases the survival rate by two folds compared with the vehicle control. The level of alanine transaminase and aspartate transaminase is consistently reduced in mice with C 87 treatment[1]. | ||||||||||||
| Name | C 87 | ||||||||||||
| CAS | 332420-90-3 | ||||||||||||
| Formula | C24H15ClN6O3S | ||||||||||||
| Molar Mass | 502.93 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ma L, et al. A novel small-molecule tumor necrosis factor α inhibitor attenuates inflammation in a hepatitis mouse model. J Biol Chem. 2014 May 2;289(18):12457-66. |