Apoptosis Activator 2

Catalog No.S2927

Apoptosis Activator 2 Chemical Structure

Molecular Weight(MW): 306.14

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 147 In stock
USD 470 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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.
Targets
Caspase-3 [1]
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%. Apoptosis Activator 2 increases the extent of caspase-3 activation at the reduced level of cyto c and caspase-3 activation by 4-fold. Apoptosis Activator 2 strongly indues caspase-3 activation, PARP cleavage, and DNA fragmentation, and finally killing cells with an IC50 of 4 μM. Apoptosis Activator 2 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. Apoptosis Activator 2 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. [1] Apoptosis Activator 2 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 Apoptosis Activator 2 (-8.1 ± 6.0%). Survival rate is not significantly altered if the other three reagents are employed (-10.7 ± 4.7%) for Apoptosis Activator 2. [2] Apoptosis activator 2 (10 μM) induces apoptosis in AGS cells as evaluated by apoptotic DNA ladder and Tunel assay. Apoptosis activator 2 (10 μM) enhances the induction of apoptosis by anti TROP2 conjugated liposomes. [3] Cyclohexamide (10 μg/mL) or zVAD (50 μM) significantly protects against Apoptosis Activator 2 toxicity in neuroneal cultures. Apoptosis activator 2 (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 Apoptosis Activator 2 toxicity in neuroneal cultures. [4]

Protocol

Kinase Assay:[1]
+ Expand

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.
Cell Research:[4]
+ Expand
  • Cell lines: Neurones
  • Concentrations: ~3 μM
  • Incubation Time: 2 hours
  • Method: All viable cells within the defined field of a microscope reticle grid are counted using a manual mechanical counter by an experimenter blinded to condition. Cells are scored viable on the basis of both positive staining with the vital dye calcein acetoxymethyl ester and the morphological criterion of a smooth, spherical soma. Counts of viable cells are made in four non-overlapping fields per culture well with each condition represented by 3 separate wells. The number of viable cells counts per well for vehicle-treated control conditions ranged from 100-200. All experiments are repeated in at least 3 independent culture preparations. Raw cell count data are statistically analyzed with one-way ANOVA, followed by between group comparisons using the Fisher LSD test (significance indicated by P < 0.05). Cell viability is presented graphically as a percentage of live cells in the vehicle-treated control condition.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (199.25 mM)
Water <1 mg/mL
Ethanol <1 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 306.14
Formula

C15H9Cl2NO2

CAS No. 79183-19-0
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID