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Procaspase-3/6 activator 1

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Chemical Structure| 1100353-03-4 同义名 : -
CAS号 : 1100353-03-4
货号 : A1339274
分子式 : C24H17N3O4
纯度 : 99%+
分子量 : 411.409
MDL号 : MFCD12020897
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 1 mg/mL(2.43 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.15mL

2.43mL

1.22mL

24.31mL

4.86mL

2.43mL
参考文献

[1]M D'Amelio,et al. Neuronal caspase-3 signaling: not only cell death. Cell Death Differ. 2010. 17(7), 1104-14.

[2]Qian Huang,et al. Caspase 3-mediated stimulation of tumor cell repopulation during cancer radiotherapy. Nat Med. 2011. 17(7), 860-6.

[3]M F Brown,et al. Loss of caspase-3 sensitizes colon cancer cells to genotoxic stress via RIP1-dependent necrosis. Cell Death Dis. 2015. 6(4), e1729.

[4]Zorn, J. A., Wolan, D. W. et al. Fibrils Colocalize Caspase-3 with Procaspase-3 to Foster Maturation. J Biol Chem. 2012. 287(40), 33781-33795.