Apoptosis Activator 2

Cas No.:	79183-19-0
Chemical Name:	1H-Indole-2,3-dione,1-[(3,4-dichlorophenyl)methyl]-
Synonyms:	1H-Indole-2,3-dione,1-[(3,4-dichlorophenyl)methyl]-;Apoptosis Activator 2;1-(3,4-Dichlorobenzyl)-1H-indole-2,3-dione;1-?(3,?4-?Dichlorobenzyl)?-?1H-?indole-?2,?3-?dione;1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione;APOPTOSIS ACTIVATOR II;Tocris-2098
SMILES:	O=C1N(CC2=CC=C(Cl)C(Cl)=C2)C3=C(C=CC=C3)C1=O
Formula:	C15H9Cl2NO2
M.Wt:	306.143
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Apoptosis Activator 2 is a potent apoptosis activator; increases procaspase-9 processing and subsequent caspase-3 activation.

In Vitro:

Apoptosis Activator 2 promotes the cytochrome c-dependent oligomerization of Apaf-1 into the mature apoptosome. Apoptosis Activator 2 exerted a cytostatic effect on the majority of cell lines tested, inhibiting cell growth by 50–100% at 10 μM in 40 of 48 cell lines tested. Apoptosis Activator 2 exerted a cytotoxic effect, reducing the cell numbers by 10–50% and 50–100% in four and eight cell lines, respectively, from the initial levels when tested at 10 μM. At 100 μM Apoptosis Activator 2 exhibited 100% cytotoxicity in virtually all cell lines, an effect that may be due to nonspecific toxicity. Of the cancer cell lines tested in the panel, cell lines of lymphoid origin (CCRF-CEM, MOLT-4, and Jurkat) were quite sensitive to compound 2-induced killing, with IC50 values ranging from 4 to 9 μM [1]. Apoptosis Activator 2 is a potent and selective carboxylesterase inhibitor with Ki of 67/31/65 nM for hiCE/hCE/rCE respectively, also has less inhibition on AChE/BChE with Ki of 48.2/12.6 uM [2].