CDK9/HDAC1/HDAC3-IN-1
Based on 1 publication(s) in Google Scholar
CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17 μM, 1.73 μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer.
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- CAS No.: 2197029-81-3
- Formula: C24H22N8OS
- Molecular Weight:470.55
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Publications Citing Use of MedChemExpress (MCE) CDK9/HDAC1/HDAC3-IN-1
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Biological Activity
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CDK9 0.17 μM (EC50) |
HDAC1 1.73 μM (IC50) |
HDAC3 1.11 μM (IC50) |
CDK9/HDAC1/HDAC3-IN-1 (Compound 13EA) (24h) shows potent anti-proliferative activities in various cancer cell lines (eg：IC50 s of 1.51 μM, 2.47 μM and 4,52 μM for HeLa, MDA-MB-231 and HepG2, respectively) [1].
CDK9/HDAC1/HDAC3-IN-1 (MDA-MB-231 cells: 0.625-5 μM, HeLa: 0.625-1.25 μM, 24 h) time- and dose-dependently inhibits p-Ser2 mRNA expression in MDA-MB-231 cells[1].
CDK9/HDAC1/HDAC3-IN-1 (MDA-MB-231 cells: 0.625-5 μM, 24 h) significantly decreases protein expression of p-Ser2 (substrate of CDK9) and simultaneously increases protein expression of Ac-H3 (substrate of HDAC) in MDA-MB-231 cells and Hela cells[1].
CDK9/HDAC1/HDAC3-IN-1 (0.625-5 μM, 24 h) concentration-dependently induces mitochondrion-related cell apoptosis, escalates the expression of cleaved PARP, and arrests cell cycle in the G2/M phase in MDA-MB-231 cells and Hela cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells, HeLa cells
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Concentration:MDA-MB-231 cells (0.625, 1.25, 2.5, 5 μM), HeLa cells (0.625, 1.25 μM)
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Incubation Time:24 h
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Result:Dose-dependently suppressed p-Ser2 (substrate of CDK9) level and upregulated Ac-H3 (substrate of HDAC) level.
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Cell Line:MDA-MB-231 cells
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Concentration:0.625, 1.25, 2.5, 5 μM
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Incubation Time:3, 6, 12, 24 h
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Result:Time- and dose-dependently downregulated CDK9 mRNA with maximal suppression at 24 h.
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Cell Line:MDA-MB-231 cells, HeLa cells
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Concentration:3 μM
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Incubation Time:24 h
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Result:Diminished p-Ser2 level and upregulated Ac-H3 level in both HeLa and MDA-MB-231 cells.
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Cell Line:MDA-MB-231 cells, HeLa cells
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Concentration:2.5 μM/3 μM
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Incubation Time:24 h
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Result:Dose-dependently decreased protein expression of Bcl-2 and Mcl-1 in MDA-MB-231 cells, and escalated protein expression of cleaved PARP in MDA-MB-231 cells and Hela cells.
Dose-dependently increased the percentage of apoptotic cells induced, ranging from 11.30 % (0.31 μM) up to 77.38 % (2.5 μM) by Annexin V-FITC/PI staining assay (HY-K1073).
Concentration-dependently decreased the mitochondrial membrane potential (MMP, Δψ) in the MDA-MB-231 cells with 17.06 %, 26.83 %, 41.97 %, and 52.73 % loss of Δψ for concentrations of 0.31, 0.63, 1.35, and 2.5 μM, respectively.
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Cell Line:MDA-MB-231 cells
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Concentration:0.31, 0.63, 1.35, and 2.5 μM
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Incubation Time:24 h
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Result:Significant increased the number of cells in the G2/M phase [ (27.43 % (0.31 μM), 79.47 % (0.63 μM), 47.58 % (1.25 μM), and 42.20 % (2.5 μM) ], and gradually promoted cells in the sub-G1 phase [(3.00 % (0.31 μM), 7.64 % (0.63 μM), 23.89 % (1.25 μM), and 27.94 % (2.5 μM)].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:female BALB/c nude mice (6 weeks old) were injected subcutaneously with log growth-phase of MDA-MB-231 cells (3 × 107 cells/mouse) [1].
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Dosage:30 mg/kg
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Administration:i.p., once a day for 10 days after tumors reaching approximately 100 mm3.
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Result:Time-dependently inhibited MDA-MB-231 xenograft tumor growth and remarkably reduced the tumor volume.
Notably increased cleaved caspase-3 level, and decreased PCNA level in the tumor tissue with IHC staining.
Chemical Information
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CAS No. 2197029-81-3
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Molecular Weight 470.55
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Formula C24H22N8OS
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SMILES
CNC1=NC(C)=C(S1)C2=NC(NC3=CC=C4C(C=C(C(NC5=CC=CC=C5N)=O)N4)=C3)=NC=C2
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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CDK9/HDAC1/HDAC3-IN-1 Related Classifications
HY-172891 Related Classifications
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