1. Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. Apoptosis Bcl-2 Family Survivin Reactive Oxygen Species (ROS)
  3. Entadamide A-CO-C12

Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer.

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Entadamide A-CO-C12

Entadamide A-CO-C12 Chemical Structure

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Description

Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer[1].

In Vitro

Entadamide A-CO-C12 (compound 3u) (48 h) exhibits antiproliferative activity against a panel of human cancer cells (MDA MB-231, DU-145, MCF-7, 4T1, NCI-H460, HepG2 and HEK-293), with IC50s of 19.11, 3.04, 2.82, 3.26, 20.98, 18.89, and 77.69 μM, respectively, showing selective anti-cancer activity in breast caner cells (MCF-7 and 4T1)[1].
Entadamide A-CO-C12 (1.5-3 μM; 48 h-5 days) suppresses migration and downregulate EMT-associated transcription factors in MCF-7 cells[1].
Entadamide A-CO-C12 (1.5-3 μM; 7 days) inhibits spheroid formation and reduces cancer stemness in MCF-7 cells[1].
Entadamide A-CO-C12 (1.5-3 μM; 24-48 h) promotes apoptosis by modulating the balance between anti-apoptotic (BCL-2, survivin) and pro-apoptotic (BAX) regulators at both the transcriptional and translational levels in MCF-7 cells, and triggers mitochondrial depolarization and activation of the intrinsic apoptotic pathway[1].
Entadamide A-CO-C12 (1.5-3 μM; 8-24 h) induces a pronounced, dose-dependent elevation in ROS production in MCF-7 cells[1].
Entadamide A-CO-C12 (1.5-3 μM; 48 h) attenuates the CD90 and CD133 levels, causes DNA damage, and triggers apoptotic nuclear condensation in MCF-7 cells in a dose-dependent manner[1].
Entadamide A-CO-C12 (1.5-3 μM; 48 h) potentiates Doxorubicin (HY-15142A) sensitivity through modulation of the ABCG2-mediated efflux pathway in MCF-7 cells[1].
Entadamide A-CO-C12 shows partial interaction with ABCB1/ABCG2 and BMI1, contributing to the modulation of drug resistance and stemness[1].

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

Cell Migration Assay [1]

Cell Line: MCF-7
Concentration: 1.5, 3 μM
Incubation Time: 0, 3, 5 days
Result: Markedly reduced cellmigration compared to the untreated control.

Apoptosis Analysis[1]

Cell Line: MCF-7
Concentration: 1.5, 3 μM
Incubation Time: 24 h
Result: Elicited a marked, concentration-dependent increase in apoptosis.
Induced 10% and 42% early apoptosis at 1.5 and 3 μM, respectively.

Real Time qPCR[1]

Cell Line: MCF-7
Concentration: 1.5, 3 μM
Incubation Time: 48 h
Result: Downregulated anti-apoptotic genes survivin, BCL-2 and upregulated pro-apoptotic genes BAX.
Demonstrated significant downregulation of the EMT-promoting transcription factors SLUG and ZEB1.
Revealed a marked downregulation of BMI1 levels.
Markedly downregulated mRNA expression of ABCG2, ABCC1, and ABCB1.
In Vivo

Entadamide A-CO-C12 (30 mg/kg, i.p., daily for 15 days from day7) exhibits potent anti-tumor activity in the 4T1 orthotopic mouse model without systemic toxicity[1].

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

Animal Model: Female-BALB/c mice (6-8 weeks old) subcutaneously injected with 4T1 murine mammary carcinoma cells[1]
Dosage: 30 mg/kg
Administration: i.p., daily for 15 days from day7
Result: Significantly inhibited tumor progression compared to control.
Showed significant size reductions relative to controls.
Showed no significant body weight changes or systemic toxicity.
Molecular Weight

357.55

Formula

C19H35NO3S

SMILES

CCCCCCCCCCCCC(OCCNC(/C=C/SC)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Entadamide A-CO-C12
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HY-179615
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