Tubulin/HDAC-IN-4
Based on 1 publication(s) in Google Scholar
Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity.
For research use only. We do not sell to patients.
- Formula: C24H26N2O6
- Molecular Weight:438.47
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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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Publications Citing Use of MedChemExpress (MCE) Tubulin/HDAC-IN-4
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Biological Activity
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HDAC1 0.73 μM (IC50) |
HDAC2 0.43 μM (IC50) |
HDAC6 0.62 μM (IC50) |
HDAC7 2.34 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
0.29 μM
Compound: 9n
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Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay
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[PMID: 38452727] |
| MCF7 | IC50 |
0.16 μM
Compound: 9n
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Cytotoxicity against human MCF7 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells incubated for 72 hrs by MTT assay
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[PMID: 38452727] |
| MDA-MB-231 | IC50 |
0.34 μM
Compound: 9n
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Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay
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[PMID: 38452727] |
| PC-3 | IC50 |
0.016 μM
Compound: 9n
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Cytotoxicity against human PC-3 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human PC-3 cells incubated for 72 hrs by MTT assay
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[PMID: 38452727] |
| U-251 | IC50 |
0.15 μM
Compound: 9n
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Cytotoxicity against human U-251 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human U-251 cells incubated for 72 hrs by MTT assay
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[PMID: 38452727] |
Tubulin/HDAC-IN-4 (compound 9n) (0-10 µM; 72 h) shows cytotoxicity with IC50s of 0.34, 0.29, 0.016, 0.15, 0.16 µM for MDA-MB-231, A549, PC-3, U251, MCF-7 cells, respectively[1].
Tubulin/HDAC-IN-4 (2.5, 5, 10, 20, 40 nM; 24 h) inhibits the colony formation of PC-3 cells in a dose-dependent manner[1].
Tubulin/HDAC-IN-4 (0.2, 1, 5, 25 µM) inhibits tubulin polymerization with an IC50 value of 4.82 µM[1].
Tubulin/HDAC-IN-4 (0.08, 0.16, 0.32; 24 h) increases the expression of Ac-α-tubulin and Ac-Histone H3 in PC-3 cells[1].
Tubulin/HDAC-IN-4 (0.08, 0.16, 0.32 µM; 24 h) induces apoptosis and cell cycle arrest at G2/M phase[1].
Tubulin/HDAC-IN-4 (0.08, 0.16, 0.32 µM; 24 h) induces a significant elevation of intracellular ROS levels[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, A549, PC-3, U251, MCF-7 cells
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Concentration:0-10 µM
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Incubation Time:72 h
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Result:Showed cytotoxicity with IC50s of 0.34, 0.29, 0.016, 0.15, 0.16 µM for MDA-MB-231, A549, PC-3, U251, MCF-7 cells, respectively.
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Cell Line:PC-3 cells
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Concentration:0.08, 0.16, 0.32 µM
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Incubation Time:24 h
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Result:Increased in both the expression of HDAC6 substrate Ac-α-tubulin and HDAC1/2/3 substrate Ac-Histone H3 in a dose-dependent manner.
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Cell Line:PC-3 cells
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Concentration:0.08, 0.16, 0.32 µM
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Incubation Time:24 h
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Result:Dose-dependently arrested PC-3 cells at G2/M phase, decreased in expression level of p-Cdc25cSer216, p-Cdc2Thr216 and p-CdcTyr15, increased the expression of Cyclin B1.
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Cell Line:PC-3 cells
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Concentration:0.08, 0.16, 0.32 µM
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Incubation Time:24 h
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Result:Induced apoptosis and increased the expression of cleaved PARP and cleaved Caspase 3, decreased the expression of Bim and Bcl-2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-week-old male BALB/c nude mouse (PC-3 cells)[1]
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Dosage:10, 20 mg/kg
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Administration:I.v.; every two days for 21 days
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Result:Inhibited the growth of tumor with the tumor growth inhibition (TGI) reached 90.07% at 20 mg/kg.
Chemical Information
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Molecular Weight 438.47
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Formula C24H26N2O6
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SMILES
CC1(C)OC2=C(C(/C=C/C3=CC=C(OC)C(NCC(NO)=O)=C3)=O)C=CC(OC)=C2C=C1
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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.
Publications (1)
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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