Apoptosis inducer 43

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Apoptosis inducer 43 is an apoptosis inducer. Apoptosis inducer 43 can induce apoptosis, SubG0-G1 cell cycle arrest, secondary necrosis, and upregulate caspase-3, p53, and Bax/Bcl-2 expression in HCT116 cells. Apoptosis inducer 43 can inhibit tumor growth in a solid Ehrlich carcinoma (SEC) mouse model. Apoptosis inducer 43 can be used to study cancers such as colon cancer, leukemia, and non-small cell lung cancer.

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Apoptosis inducer 43 Chemical Structure

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Caspase 3

Bcl-2

Bax

In Vitro

Apoptosis inducer 43 (Compound 5f) (10 μM) shows anticancer activity and demonstrates an average inhibition percentage exceeding 80% and an average GI₅₀ below 5 μM against NCI 60 cells (leukemia, non-small cell lung, colon, central nervous system, melanoma, ovarian, renal prostate, and breast cancer)^[1].
Apoptosis inducer 43 (1.79-10 μM, 24 h) induces cell cycle arrest, primarily at the SubG0/G1 phase, induces apoptosis in HCT-116 cells ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	HCT-116 cells
Concentration:	10 μM
Incubation Time:	24 h
Result:	Induced changes in cell cycle distribution, leading to cell cycle arrest in the SubG0-G1 phase, with the percentage of cells in the G0/G1 cycle increasing from 7% (control sample) to 44%. Resulted in reduction of the percentage of cells in the remaining phases, G0-G1, S and G2/M.

Apoptosis Analysis^[1]

Cell Line:	HCT-116 cells
Concentration:	1.79 μM
Incubation Time:	24 h
Result:	Decreased the percentage of live cells and increased the proportion of necrotic cells. Increased the levels of caspase-3, p53, and Bax proteins, and decreased the level of Bcl-2 protein.

In Vivo

Apoptosis inducer 43 (Compound 5f) (10 mg/kg, i.p., three times weekly, 14 days) demonstrates antitumor effects in solid ehrlich carcinoma (SEC) mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SEC (0.2 mL/mouse) female Swiss albino mice (18-22g) model^[1]
Dosage:	10 mg/kg
Administration:	i.p., three times weekly, 14 days
Result:	Demonstrated antitumor effects, resulting in a 72.5% reduction in tumor volume and a 76% reduction in tumor weight. Showed small foci of tumor cells with distinct mitotic figures were surrounded by large areas of necrosis. Reduced mitotic cell counts and VEGF expression.

Molecular Weight

560.56

Formula

C₃₂H₂₇F₃N₂O₄

SMILES

O=C(NC1=CC=CC(C(/C=C/C2=CC=C(C3=CC=CC=C3)C=C2)=O)=C1)C([NH3+])CC4=CC=CC=C4.FC(F)(F)C([O-])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. El-Haggar R, et al.. Amino acid-modified chalcone derivatives with in vitro and in vivo efficacy against colon cancer. Eur J Med Chem. 2025 Nov 5;297:117963. https://pubmed.ncbi.nlm.nih.gov/40695035/ [Content Brief]