HDAC6-IN-67
HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2196247-20-6
- Formula: C17H15N3O3
- Molecular Weight:309.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
HDAC6-IN-67 shows significant time-dependent inhibition of tumor cells in all tested human cancer cell lines, with GI50 values ranging from 2.9 to 24.8 μM, it also shows strong anti-proliferative activity against MCF-7/ADR cells after 72 hours (GI50 = 2.4 μM)[1].
HDAC6-IN-67 (0.01-2 μM, 24 hours) can dose-dependently increase the acetylation of α-tubulin in MCF-7/ADR cells without affecting the acetylation of histone H3 even at high concentrations [1].
HDAC6-IN-67 (0.1-2 μM, 10 days) results in a significant dose-dependent inhibition of colony formation in MCF-7/ADR cells[1].
HDAC6-IN-67 (0.1-2 μM, 24 h) significantly induces early and late apoptosis, and further confirms its apoptotic effect, demonstrating a dose-dependent induction of cleavage of Caspase 9, Caspase 8, Caspase 3, and PARP, along with significant upregulation of the pro-apoptotic protein Bax and downregulation of the anti-apoptotic protein Bcl-2 in MCF-7/ADR 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/ADR cells
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Concentration:0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Dose-dependently increased the acetylation of α-tubulin.
Induced α-tubulin acetylation at concentrations as low as 0.1 μM, without affecting the acetylation of Histone H3 even at concentrations up to 1 μM.
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Cell Line:MCF-7/ADR cells
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Concentration:0.1 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:10 days
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Result:Resulted in a significant dose-dependent inhibition of colony formation.
A concentration of 1 μM was able to suppress colony formation by approximately 65 %.
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Cell Line:MCF-7/ADR cells
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Concentration:0.1 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:24 h
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Result:Significantly induces early and late apoptosis by 25.4% and 15.7%.
The cleavage of Caspase 9, Caspase 8, Caspase 3, and PARP were significantly induced in a dose-dependent manner.
The apoptotic protein Bax was significantly induced, whereas the anti-apoptotic protein Bcl-2 was remarkably decreased in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Subcutaneously injecting nude mice with HCT116 human colon cancer cells (2.0 × 106 cells/ mice).
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Dosage:5 mg/kg, 10 mg/kg
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Administration:I.p., daily during weekdays, followed by weekend rest for 17 days
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Result:Showed delayed tumor growth starting right after the first measurement.
Found no differences in body weight, treatment-related deaths, or abnormal behaviors between the control and experimental groups.
Chemical Information
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CAS No. 2196247-20-6
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Molecular Weight 309.32
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Formula C17H15N3O3
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SMILES
CC1=NC2=C(C(N1CC3=CC=C(C=C3)C(NO)=O)=O)C=CC=C2
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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)