HDAC-IN-91
HDAC-IN-91 is a multiple inhibitor of HDAC (IC50 = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (Ki = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC50 = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research.
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- Fòrmula: C23H21BrN2O5S
- Peso molecular:517.39
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HDAC1 134.22 nM (IC50) |
HDAC2 66.29 nM (IC50) |
CA IX 72.03 nM (Ki) |
CA XII 50.76 nM (Ki) |
Bax |
Bcl-2 |
Caspase-9 |
Caspase-7 |
In Vitro
HDAC-IN-91 (Compounds 6e) shows cytotoxicity against MCF7, Hela, HCT116, A549 cells, with IC50s of 1.40 μM, 2.22 μM, 1.57 μM, 2.54 μM, respectively[1].
HDAC-IN-91 presents promising inhibitory activity against HDAC isoforms 3, 4, 6, and 8 with IC50s ranging between 100 and 900 nM[1].
HDAC-IN-91 (1.40 μM, 48 h) inhibits the growth of MCF-7 cells by interfering with cell mitosis and ultimately inducing cell apoptosis[1].
HDAC-IN-91 (1.40 μM, 48 h) induces apoptosis by increasing the Bax/Bcl-2 ratio and caspase-9 and -7 levels in MCF-7 cells[1].
HDAC-IN-91 (1.40 μM, 48 h) has potential PARP1 inhibitory activity in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:1.40 μM
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Incubation Time:48 h
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Result:Reduced the cell population in the S phase (DNA synthesis phase) to 22.3%, reduced the G0-G1 phase (non-proliferating cell ratio) to 31.6%.
Increased the proportion in the G2/M phase to 46.1, caused significant cell death, and increased the number of cells in the Sub-G1 phase to 42.09%.
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Cell Line:MCF-7 cells
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Concentration:1.40 μM
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Incubation Time:48 h
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Result:Induced apoptosis in breast cancer cells with an apoptotic rate of 26.75 and induced necrotic cell death of 15.36.
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Cell Line:MCF-7 cells
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Concentration:1.40 μM
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Incubation Time:48 h
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Result:Increased Bax protein levels to 391.6 Pg/mL, decreased Bcl-2 protein levels to 2.11 ng/mL, increased the Bax/Bcl-2 ratio, increased Caspase-9 and Caspase-7 protein levels to 13.57 ng/mL and 2.62 ng/mL, respectively, and decreased PARP1 to 73.92 ng/mL, suggesting potential PARP1 inhibitory activity.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Cell Cytotoxicity Assay
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Peso molecular 517.39
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Fòrmula C23H21BrN2O5S
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SMILES
BrC1=CC=C(C(/C=C/C2CC=C(OCC(NC3=CC=C(S(N)(=O)=O)C=C3)=O)C=C2)=O)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-91 Related Classifications
HY-175021 Related Classifications
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