HDAC1/6-IN-3
HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3038691-85-6
- Formula: C24H27N3O4S
- Molecular Weight:453.55
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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
- Purity & Documentation
- References
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Help & FAQs
All Caspase Isoforms
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Biological Activity
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HDAC1 1.1 nM (IC50) |
HDAC6 2.7 nM (IC50) |
HDAC1/6-IN-3 (Compound 15a) (72 h)shows excellent inhibitory activities against HepG2 (IC50 = 0.12 μM), PC9 (IC50 = 0.53 μM), HCT116 (IC50 = 1.12 μM) and MCF7 cell (IC50 = 3.12 μM)[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) increases the level of acetyl-H3 and H4 in a dose-dependent manner in HepG2 cells[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 10-14 d) suppresses the formation of colonies of HepG2 cells in a dose-dependent manner.[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 24 h) induces G0/G1 arrest in HepG2 cells may be correlated the downregulation of with CDK4 and Cyclin D1 proteins[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 48 h) enhances ROS generation and DNA damage accumulation to induce apoptosis in HepG2 cells[1].
HDAC1/6-IN-3 (0.2-0.5 μM, 24-48 h) triggers pyroptosis in HepG2 cells through caspase-3 cleavage of GSDME[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells
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Concentration:0.2 and 0.5 μM
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Incubation Time:24 h
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Result:Significantly inhibited HepG2 cells in G0/G1 phase in a dose-dependent manner.
The G2/M ratio decreased from 25.34 to 22.85% and the S-phase value decreased from 32.99 to 13.72%.
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Cell Line:HepG2 cells
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Concentration:0.2 and 0.5 μM
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Incubation Time:48 h
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Result:Induced apoptosis in 28.2% at 0.2 µM and 46.5% at 0.5 µM.
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Cell Line:HepG2 cells
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Concentration:0.2 and 0.5 μM
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Incubation Time:24 h
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Result:Dose-dependently increased the ROS levels.
Showed dose-dependent γH2AX foci formation.
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Cell Line:HepG2 cells
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Concentration:0.2 and 0.5 μM
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Incubation Time:24 h
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Result:Increased the levels of acetyl-H3 and H4 in a dose-dependent manner.
Down-regulated the expression of Cyclin D1 and CDK4.
Upregulated the expression of Cl-PARP, Cl-caspase 3 in a dose-dependent manner.
Resulted in elevated levels of the N-terminal fragment of gasdermin E (GSDME) and caspase-3.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HepG2 induced xenograft model established in male BALB/c nude mice[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.), twice a week for 3 weeks
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Result:Dose-dependently inhibited the growth of tumors.
Observed a dose-dependent reduction in Ki67 immunostaining.
Induced the increase of Ac- H3/H4､Cl-caspase3 and GSDME-N in a dose-dependent manner.
Chemical Information
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CAS No. 3038691-85-6
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Molecular Weight 453.55
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Formula C24H27N3O4S
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SMILES
O=C(NO)CCCCCC(N(C1=CC=C(OC)C=C1)CC2=CSC(C3=CC=CC=C3)=N2)=O
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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)
HDAC1/6-IN-3 Related Classifications
HY-175176 Related Classifications
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