Bcl-2/Mcl-1-IN-5
Bcl-2/Mcl-1-IN-5 (Compound S6) is a Bcl-2 and Mcl-1 inhibitor. Bcl-2/Mcl-1-IN-5 promotes Apoptosis, downregulates anti-apoptotic proteins Bcl-2 and Mcl-1, induces mitochondrial membrane potential depolarization, and activates the Caspase-dependent apoptotic cascade, as evidenced by Caspase-3 activation and PARP1 cleavage. Bcl-2/Mcl-1-IN-5 has anti-hepatocellular carcinoma activity.
For research use only. We do not sell to patients.
- Formula: C38H42BrN5O2
- Molecular Weight:680.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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PARP1 |
Caspase-3 |
Bcl-2 |
Mcl-1 |
Bcl-2/Mcl-1-IN-5 potently inhibits the proliferation of Huh-7, MHCC-97H, and HepG2 human HCC cell lines with IC50 values of 9.13 ± 0.29 μM, 6.76 ± 0.06 μM, and 15.9 ± 0.98 μM, respectively, and has reduced toxicity to normal HL7702 hepatocytes[1].
Bcl-2/Mcl-1-IN-5 (2-8 μM; 14 days with replenishment every 3 days) suppresses the long-term clonogenic survival of MHCC-97H human HCC cells, with 8 μM treatment reducing colony formation by approximately 71%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human MHCC-97H HCC cell line
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Concentration:2, 4, 8 μM
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Incubation Time:24 h
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Result:Upregulated pro-apoptotic Bax protein in a dose-dependent manner.
Downregulated anti-apoptotic Bcl-2, Mcl-1, and Bcl-xL proteins in a dose-dependent manner.
Markedly increased the Bax/Bcl-2 ratio.
Induced caspase-3 activation and PARP1 cleavage, as shown by increased levels of active caspase-3 and cleaved PARP.
Chemical Information
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Molecular Weight 680.68
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Formula C38H42BrN5O2
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SMILES
O=C(N([C@@H]1CC(N2C[C@@H]3CCCN4CCC[C@H]([C@H]2C1)[C@H]34)=O)CCC5=NC=CC=C5)C6=CN(C7=C6C=CC=C7)CC8=CC=C(C=C8)Br
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bcl-2/Mcl-1-IN-5 Related Classifications
HY-181746 Related Classifications
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