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Apoptosis Activator 2 Caspase activator

Cat.No.S2927

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.
Apoptosis Activator 2 Caspase activator Chemical Structure

Chemical Structure

Molecular Weight: 306.14

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Quality Control

Batch: S292701 DMSO]61 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.58%
  • Cited in Nature Medicine for its top-tier quality
  • COA
  • NMR
  • HPLC
  • SDS
  • Datasheet
99.58

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (199.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 306.14 Formula

C15H9Cl2NO2

 Storage (From the date of receipt)
CAS No. 79183-19-0 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=C2C(=C1)C(=O)C(=O)N2CC3=CC(=C(C=C3)Cl)Cl

Mechanism of Action

Targets/IC50/Ki
Caspase-3
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%. This compound increases the extent of caspase-3 activation at the reduced level of cyto c and caspase-3 activation by 4-fold. It strongly indues caspase-3 activation, PARP cleavage, and DNA fragmentation, and finally killing cells with an IC50 of 4 μM. This activator 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. It 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. This chemical 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 this compound (-8.1 ± 6.0%). Survival rate is not significantly altered if the other three reagents are employed (-10.7 ± 4.7%) for this activator. This compound (10 μM) induces apoptosis in AGS cells as evaluated by apoptotic DNA ladder and Tunel assay. It (10 μM) enhances the induction of apoptosis by anti TROP2 conjugated liposomes. Cyclohexamide (10 μg/mL) or zVAD (50 μM) significantly protects against this chemical toxicity in neuroneal cultures. This activator (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 this compound toxicity in neuroneal cultures.
Kinase Assay
Cell-Free Apoptosis Assay
HeLa cell cytoplasmic extracts are prepared according to previously published reports. Apoptosis Activator 2 in DMSO are distributed into 96-well microtiter plates at a final concentration of 1 mM (final DMSO concentration is 1% vol/vol). To each well is added 250 μg of total protein from cytoplasmic extracts in HEB buffer (50 mM Hepes, pH 7.4/50 mM KCl/5 mM EGTA/2 mM MgCl), with 2 mM DTT, 2 μM cyto c, and 0.5 μM DEVD-AFC (Asp-Glu-Val-Asp-7-amino-4-trifluoromethylcoumarin) substrate in a total of 150 μL. Plates are incubated at 37 ℃, and fluorescence is read in a LJL Biosystems plate reader at 10-min intervals.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/20561156/

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