Apoptosis Activator 2

Catalog #
27733-1
$230 *
Size: 10 mg
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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.

Synonyms
Apoptosis Activator II; AG-H-17727; ZINC02276110; 1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione
Product Info
Storage and Usage
Citations
Target(s)
Caspase
Formula
C15H9Cl2NO2
MW
306.1 Da
Solubility
Soluble in DMSO (5 mg/ml), methanol (5 mg/ml), and ethanol.
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 Registry #
79183-19-0
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).
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.