Description
Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells.
Chemical Name
1H-Indole-2,3-dione, 1-[(3,4-dichlorophenyl)methyl]-
In vitro
Apoptosis Activator 2 (20 μM) at the reduced cyto c concentration increases the fraction of Apaf-1 in the apoptosome by 1.5-fold to 33%. Apoptosis Activator 2 increases the extent of caspase-3 activation at the reduced level of cyto c and caspase-3 activation by 4-fold. Apoptosis Activator 2 strongly indues caspase-3 activation, PARP cleavage, and DNA fragmentation, and finally killing cells with an IC50 of 4 μM. Apoptosis Activator 2 induces apoptosis of PBL, HUVEC, Jurkat, Molt-4, CCRF-CEM, BT-549, MDA-MB-468 and NCI-H23 with of IC50 of 50 μM, 43 μM, 4 μM, 6 μM, 9 μM, 20 μM, 44 μM and 35 μM. Apoptosis Activator 2 exerts a cytostatic effect on the majority of tumor cell lines tested, inhibiting cell growth by 50-100% at 10 μM in 40 of 48 cell lines tested. Apoptosis Activator 2 induces cell death by triggering apoptosome formation. The level of En1 expression does not have a significant influence on the survival rates of Ventral midbrain cultures for Apoptosis Activator 2 (-8.1 ± 6.0%). Survival rate is not significantly altered if the other three reagents are employed (-10.7 ± 4.7%) for Apoptosis Activator 2.Apoptosis activator 2 (10 μM) induces apoptosis in AGS cells as evaluated by apoptotic DNA ladder and Tunel assay. Apoptosis activator 2 (10 μM) enhances the induction of apoptosis by anti TROP2 conjugated liposomes.Cyclohexamide (10 μg/mL) or zVAD (50 μM) significantly protects against Apoptosis Activator 2 toxicity in neuroneal cultures. Apoptosis activator 2 (3 μM) results in numerous neurones with pyknotic nuclei suggestive of cell death involving apoptosis. DHT (10 nM) or E2 (10 nM) significantly protects against Apoptosis Activator 2 toxicity in neuroneal cultures.
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