Apoptosis Activator 2

Catalog 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.

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In DMSO USD 190 In stock
USD 147 In stock
USD 470 In stock
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Apoptosis Activator 2 Chemical Structure

Apoptosis Activator 2 Chemical Structure
Molecular Weight: 306.14

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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 Assay: [4]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Nguyen JT, et al. Proc Natl Acad Sci U S A, 2003, 100(13), 7533-7538.

[2] Alavian KN, et al. Neural Dev, 2009, 16(4), 11.

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Chemical Information

Download Apoptosis Activator 2 SDF
Molecular Weight (MW) 306.14
Formula

C15H9Cl2NO2

CAS No. 79183-19-0
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 61 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <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 Name 1H-Indole-2,3-dione, 1-[(3,4-dichlorophenyl)methyl]-

Research Area

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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