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) .
CAS Number: 79183-19-0
Molecular Weight: 306.14
Chemical Name: 1-[(3,4-dichlorophenyl)methyl]-1H-indole-2,3-dione
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
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 .
- 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.
- Hyatt JL, et al. Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. J Med Chem. 2007 Apr 19;50(8):1876-85.
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