|N-(3-(咪唑并[1,2-a]吡啶-2-基)苯基)-8-甲氧基-2-氧代-2H-苯并吡喃-3-酰胺|CsnPharm

CAS No.: 1100353-03-4

CASP3 Activator 1541 is an activator of procaspase-3.

规格	价格	促销价格	库存	数量

400-920-2911

加入购物车大规格询价

产品咨询

400-920-2911

纯度 & 质量文件批次:

生物活性

描述Caspases are a family of cysteinyl aspartate-specific proteases that are highly conserved in multicellular organisms and function as central regulators of apoptosis. A member of this family, caspase-3, has been identified as a key mediator of apoptosis in neuronal cells^[1]. One downstream effector that caspase 3 regulates is prostaglandin E(2) (PGE(2)), which can potently stimulate growth of surviving tumor cells. Deficiency of caspase 3 either in tumor cells or in tumor stroma caused substantial tumor sensitivity to radiotherapy in xenograft or mouse tumors. In human subjects with cancer, higher amounts of activated caspase 3 in tumor tissues are correlated with markedly increased rate of recurrence and death^[2]. Caspase-3 knockout (C3KO) and knockdown human colorectal cancer cells, and found that they are unexpectedly sensitized to DNA-damaging agents including 5-fluorouracil (5-FU), etoposide, and camptothecin. C3KO xenograft tumors also displayed enhanced therapeutic response and cell death to 5-FU.^[3]. CASP3 Activator 1541 is an activator of the proenzyme forms of caspase-3, which can induce cell death. Compound 1541 self-assembles into nanofibrils, and localization of procaspase-3 to the fibrils promotes activation. Experiment showed that fibril-induced colocalization of trace amounts of caspase-3 or other initiator proteases with procaspase-3 dramatically stimulates maturation of the proenzyme in vitro^[4].
参考文献

实验方案

技术信息

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

请登录您的专属账户