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Background: Apoptosis Activator 2 is a cell-permeable indoledione compound that activates caspases in a cytochrome c-dependent manner and induces apoptosis in tumor cells by promoting the oligomerization of Apaf-1 into the mature apoptosome. Its cytotoxicity is selective towards tumor cells (IC50 < 10 µM for Jurkat, Molt-4, and CCRF-CEM). Apoptosis Activator 2 shows little or no effect on non-tumor cells or cells that are deficient in caspase-3 or Apaf-1 (IC50 > 40 µM). Through the induction of apoptosis, Apoptosis Activator 2 notably induces caspase-3 activation, PARP cleavage and DNA fragmentation. Moreover, this induction of apoptosis only occurs in tumor cell lines (such as breast, lung, colon, and epidermal cancer cell lines).
Biological Activity: Induces apoptosis of tumor cell lines, including BT-549: IC50 = 20 µM; NCI-H23: IC50 = 35 µM; Jurkat: IC50 = 4 µM; Molt-4: IC50 = 6 µM; and CCRF-CEM: IC50 = 9 µM.
CAS Number: 79183-19-0
Description: Apoptosis Activator 2 is a small, cell permeable activator of caspase-3. Apoptosis Activator 2 induces apoptosis specifically in tumor cell lines, but not normal cell lines, with IC50 value of about 4 µM.
Solubility: Soluble in DMSO (5 mg/ml), methanol (5 mg/ml), and ethanol.
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: Caspase
Biosafety Level: Not applicable (BSL-1)
References: 1. Nguyen JT, Wells JA. Proc Natl Acad Sci U S A. 2003 Jun 24;100(13):7533-8.
2. Nguyen TV, et al. J Neuroendocrinol. 2010 Sep;22(9):1013-22.