HDAC6-IN-74
HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.
For research use only. We do not sell to patients.
- Formula: C16H17N3OSSe
- Molecular Weight:378.35
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC6 0.036 μM (IC50) |
HDAC1 3.0 μM (IC50) |
HDAC2 2.3 μM (IC50) |
HDAC3 4.9 μM (IC50) |
HDAC4 2.1 μM (IC50) |
HDAC5 8.4 μM (IC50) |
HDAC10 1.7 μM (IC50) |
HDAC11 6.4 μM (IC50) |
HDAC6-IN-74 (compound 14a) (0.05-50.0 μM; 72 h) potently inhibits the proliferation of HepG2 hepatocellular carcinoma cells with an IC50 of 0.7 μM, shows low activity against Huh7 cells, exhibits no activity against LM3 cells, and has high selectivity for tumor cells relative to non-tumorigenic cell lines[1].
HDAC6-IN-74 (1-10 μM; 0-72 h) induces apoptosis and S-phase cell cycle arrest, and inhibits cell invasion and migration in HepG2 cells[1].
HDAC6-IN-74 (0-10.0 μM; 24 h) downregulates the expressions of HDAC6 and p-ERK1/2, and upregulates the expressions of Ac-H3 and Ac-α-tubulin in HepG2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2, Huh7, LM3, THLE-2
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Concentration:50.0, 25.0, 10.0, 5.0, 2.5, 1.0, 0.5, 0.1 and 0.05 μM
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Incubation Time:72 h
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Result:Exhibited an IC50 of 0.7 μM against HepG2 cells, 9.4 μM against Huh7 cells, >50 μM against LM3 cells, >50 μM against THLE-2 cells.
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Cell Line:HepG2
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Concentration:1 μM, 10 μM
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Incubation Time:72 h
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Result:Induced an apoptotic rate of 19.48% at 1 μM.
Induced an apoptotic rate of 25.73% at 10 μM.
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Cell Line:HepG2
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Concentration:0, 0.5, 1.0, 2.5, 5.0 and 10.0 μM
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Incubation Time:24 h
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Result:Significantly reduced HDAC6 and p-ERK1/2 protein levels at 2.5 μM.
Dose-dependently increased Ac-H3 and Ac-α-tubulin protein levels without affecting total H3 or α-tubulin levels at concentrations from 0.5 to 10.0 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice treated HepG2 (female, 6-week-old)[1]
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Dosage:12.5 mg/kg; 25.0 mg/kg
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Administration:Intragastric administration.; every other day; 24 days
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Result:Achieved a 47.6% tumor inhibition rate, significantly reduced HDAC6 protein levels in tumor tissue, significantly increased Ac-α-tubulin protein levels in tumor tissue, and induced tumor cell apoptosis at 12.5 mg/kg.
Achieved a 90.2% tumor inhibition rate, caused a more significant reduction in HDAC6 protein levels in tumor tissue compared to the 12.5 mg/kg dose, increased Ac-α-tubulin protein levels to ~15.4-fold that of the control group, and induced the highest level of tumor cell apoptosis among the treatment groups at 25 mg/kg.
Caused no obvious changes in mouse body weight or histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney).
Chemical Information
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Molecular Weight 378.35
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Formula C16H17N3OSSe
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SMILES
O=C(NC1=NC=C(C2=CC=CC=C2)S1)CCCCC[Se]C#N
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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)
HDAC6-IN-74 Related Classifications
HY-181579 Related Classifications
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