HDAC1-IN-13
HDAC1-IN-13 is an orally active HDAC1 inhibitor with IC50 values of 91, 185, 170, and 280 nM against HDAC1, HDAC2, HDAC3, and HDAC10, respectively, and shows no activity against HDAC4, HDAC5, HDAC6, HDAC7, and HDAC9. HDAC1-IN-13 induces extrinsic apoptosis by activating the caspase-8 pathway and triggers G0/G1 cell cycle arrest. HDAC1-IN-13 can be used for the research of leukemia.
For research use only. We do not sell to patients.
- CAS No.: 3053289-22-5
- Formula: C23H20N4O
- Molecular Weight:368.43
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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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All Caspase Isoforms
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Biological Activity
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HDAC1 91 nM (IC50) |
HDAC2 181 nM (IC50) |
HDAC3 170 nM (IC50) |
HDAC10 280 nM (IC50) |
Caspase-8 |
HDAC1-IN-13 (Compound 6B) potently inhibits HDAC1 (IC50 = 91 nM), HDAC2 (IC50 = 185 nM), HDAC3 (IC50 = 170 nM), and HDAC10 (IC50 = 280 nM) enzymes, with no activity against HDAC4, HDAC5, HDAC7, HDAC8, or HDAC9[1].
HDAC1-IN-13 (Compound 6B) (72 h) potently inhibits the proliferation of HL-60 (IC50 = 0.31 μM), CCRF-CEM (IC50 = 0.36 μM), and HepG2 (IC50 = 1.01 μM) cancer cells in vitro[1].
HDAC1-IN-13 (Compound 6B) (72 h) has low cytotoxicity to LO2 normal human hepatocytes (IC50 = 5.67 μM) and a high selectivity index of 18.3 relative to HL-60 cancer cells[1].
HDAC1-IN-13 (Compound 6B) (0.1-2.5 μM; 48 h) concentration-dependently increases histone H3 acetylation, downregulates Rb/p-Rb and caspase-8 precursor, and modulates BAX, BAK, and BCL-2 expression in HL-60 cells after 48 h of treatment[1].
HDAC1-IN-13 (Compound 6B) (0-2.5 μM; 48 h) concentration-dependently induces apoptosis in HL-60 cells, with a 46.1% apoptosis rate following 48 h treatment with 2.5 μM[1].
HDAC1-IN-13 (Compound 6B) (0-2.5 μM; 48 h) concentration-dependently induces G0/G1 phase cell cycle arrest in HL-60 cells, with 76.5% of cells arrested in G0/G1 following 48 h treatment with 2.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60 promyelocytic leukemia cells
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Concentration:0.1 μM, 0.5 μM, 2.5 μM
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Incubation Time:48 h
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Result:Induced a concentration-dependent increase in acetylated histone H3 (Ac-H3) levels, while total histone H3 levels remained unchanged.
Downregulated expression of Rb, phosphorylated Rb (p-Rb), and caspase-8 precursor in a concentration-dependent manner.
Downregulated BAX, BAK, and BCL-2 expression.
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Cell Line:HL-60 promyelocytic leukemia cells
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Concentration:0 μM, 0.1 μM, 0.5 μM, 2.5 μM
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Incubation Time:48 h
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Result:Induced apoptosis in a concentration-dependent manner, with apoptosis rates of 13.87% (0 μM), 25.6% (0.1 μM), 27.6% (0.5 μM), and 46.1% (2.5 μM).
Reached a late apoptotic cell proportion of 22.7% at the highest concentration.
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Cell Line:HL-60 promyelocytic leukemia cells
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Concentration:0 μM, 0.1 μM, 0.5 μM, 2.5 μM
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Incubation Time:48 h
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Result:Induced G0/G1 phase cell cycle arrest in a concentration-dependent manner, with the proportion of cells in G0/G1 phase increasing from 56.4% (0 μM) to 76.5% (2.5 μM).
HDAC1-IN-13 (20 mg/kg; i.p.; once daily; for 7 consecutive days) exhibits potent in vivo anti-leukemia activity with no obvious toxicity in mouse models following intraperitoneal administration[1].
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 (male, 6-8 weeks old, 18-22 g, subcutaneous xenograft model)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.g.; daily; 18 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 20.72% at 30 mg/kg.
Showed no obvious pathological changes in heart, liver, spleen, lung, or kidney tissue.
Maintained stable mouse body weights throughout the study.
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Animal Model:BALB/c nude (male, 6-8 weeks old, 18-22 g, subcutaneous xenograft model)[1]
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Dosage:20 mg/kg
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Administration:i.p.; daily; 7 days
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Result:Reduced tumor volume by 58.4% after 7 days.
Showed no changes in mouse body weight during the study, indicating low in vivo toxicity.
Chemical Information
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CAS No. 3053289-22-5
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Molecular Weight 368.43
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Formula C23H20N4O
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SMILES
O=C(NC1=CC=CC=C1N)C(C=C2)=CC=C2CNC3=CC=NC4=CC=CC=C43
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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)
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