Apoptosis Activator 2

MDK83190, also known as Apoptosis Activator 2, is an Apoptosis Activator. MDK83190 has CAS#79183-19-0, in which the last 5 digit was used for its name for easier communication. MDK83190 has been shown to induce apoptosis in leukemia cells (IC50 = 4-9 μM) .

Product information

CAS Number: 79183-19-0

Molecular Weight: 306.14

Formula: C15H9Cl2NO2

Chemical Name: 1-[(3,4-dichlorophenyl)methyl]-1H-indole-2,3-dione

Smiles: O=C1C2=CC=CC=C2N(CC2=CC(Cl)=C(Cl)C=C2)C1=O

InChiKey: KGRJPLRFGLMQMV-UHFFFAOYSA-N

InChi: InChI=1S/C15H9Cl2NO2/c16-11-6-5-9(7-12(11)17)8-18-13-4-2-1-3-10(13)14(19)15(18)20/h1-7H,8H2

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: ≥ 46 mg/mL

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

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. 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 .

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.

Products are for research use only. Not for human use.