Apoptosis Activator 2

Modify Date: 2024-01-02 19:37:55

Apoptosis Activator 2 Structure
Apoptosis Activator 2 structure
Common Name Apoptosis Activator 2
CAS Number 79183-19-0 Molecular Weight 306.143
Density 1.5±0.1 g/cm3 Boiling Point 470.6±55.0 °C at 760 mmHg
Molecular Formula C15H9Cl2NO2 Melting Point N/A
MSDS N/A Flash Point 238.4±31.5 °C

 Use of Apoptosis Activator 2


Apoptosis Activator 2 is a potent apoptosis activator; increases procaspase-9 processing and subsequent caspase-3 activation.IC50 value: 4-9 uM(Leukemia origin cells)[1]Target: Apoptosis activatorin 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].

 Names

Name 1-[(3,4-dichlorophenyl)methyl]indole-2,3-dione
Synonym More Synonyms

 Apoptosis Activator 2 Biological Activity

Description Apoptosis Activator 2 is a potent apoptosis activator; increases procaspase-9 processing and subsequent caspase-3 activation.IC50 value: 4-9 uM(Leukemia origin cells)[1]Target: Apoptosis activatorin 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].
Related Catalog
References

[1]. Nguyen JT, et al. Direct activation of the apoptosis machinery as a mechanism to target cancer cells. Proc Natl Acad Sci U S A. 2003 Jun 24;100(13):7533-8.

[2]. Hyatt JL, et al. Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. J Med Chem. 2007 Apr 19;50(8):1876-85.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 470.6±55.0 °C at 760 mmHg
Molecular Formula C15H9Cl2NO2
Molecular Weight 306.143
Flash Point 238.4±31.5 °C
Exact Mass 305.001038
PSA 37.38000
LogP 3.42
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.671
Storage condition Store at RT

 Safety Information

Safety Phrases 24/25
RIDADR 3077
HS Code 29145090

 Synonyms

1H-Indole-2,3-dione, 1-[(3,4-dichlorophenyl)methyl]-
Apoptosis Activator 2
Apoptosis Activator II
Tocris-2098
1-(3,4-Dichlorobenzyl)-1H-indole-2,3-dione
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