HDAC1/2 and CDK2-IN-1
HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity.
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- CAS No.: 2418559-01-8
- Formula: C26H22ClN7O
- Molecular Weight:483.95
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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
Biological Activity
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HDAC1 70.7 nM (IC50) |
HDAC2 23.1 nM (IC50) |
CDK2 0.80 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.47 μM
Compound: 14d
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Antiproliferative activity against human A-375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A-375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 32361064] |
| HCT-116 | IC50 |
0.58 μM
Compound: 14d
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 32361064] |
| HeLa | IC50 |
1.05 μM
Compound: 14d
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Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 32361064] |
| HepG2 | IC50 |
0.86 μM
Compound: 14d
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Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 32361064] |
| NCI-H460 | IC50 |
1.59 μM
Compound: 14d
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Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
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[PMID: 32361064] |
HDAC1/2 and CDK2-IN-1 (compound 14d) shows excellent antiproliferative activities against H460, A375, HepG2, HCT116 and Hela cells with IC50 values of 1.59, 0.47, 0.86, 0.58 and 1.05 μM, respectively[1].
HDAC1/2 and CDK2-IN-1 (0.5 μM, 48 h) significantly inhibits the migration of H460 and A375 cells[1].
HDAC1/2 and CDK2-IN-1 (0-2 μM, 24 h) significantly blocks the cell cycle in the G2/M phase[1].
HDAC1/2 and CDK2-IN-1 (0-2 μM, 48 h) promotes cancer cell apoptosis in a dose-dependent manner[1].
HDAC1/2 and CDK2-IN-1 (1 μM, 12 h) inhibits CDK2 and HDAC activity, causing cancer cell death[1].
HDAC1/2 and CDK2-IN-1 (1 μM, 24 h) strongly increases ROS levels in A375 cells, causes cancer cell death by improving 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:A375, HCT116, H460 and Hela cells[1]
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Concentration:0, 0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Significantly blocked the cell cycle, induced a loss of G0/G1 phase cells and an increase of G2/M phase cells, led to an apparent accumulation of cells in G2/M phase at 0.5 μM (A375, the percentage from 13.70 to 57.03%; HCT116, from 27.46 to 76.99%; Hela, from 7.89% to 51.85%).
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Cell Line:A375, HCT116, H460 and Hela cell lines[1]
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Concentration:0, 0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Promoted cancer cell apoptosis in a dose-dependent manner, with the apoptosis rates of 91.99% (A375), 89.60% (HCT116), 59.10% (H460), and 22.36% (Hela) respectively at the concentration of 2 μM.
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Cell Line:A375 cells[1]
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Concentration:1 μM
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Incubation Time:12 h
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Result:Significantly inhibited CDK2 and increased the acetylation level of histone H3, inhibited CDK2 and HDAC activity, causing cancer cell death.
HDAC1/2 and CDK2-IN-1 (compound 14d) (ICR mice; 4 mg/kg, IV; 20 mg/kg, IP) exhibits desirable pharmacokinetic properties[1].
Pharmacokinetic Parameters of HDAC1/2 and CDK2-IN-1 in male ICR mice[1].
| Dose (mg/kg) | 4 | 20 |
| Administration | IV | IP |
| T1/2 (h) | 1.48 | 2.84 |
| Tmax (h) | 2 | |
| Cmax (ng/mL) | 1360 | |
| AUC0-t (ng/mL*h) | 2850 | 7240 |
| MRT0-t (h) | 0.563 | 4.54 |
| CL (mL/(min/kg)) | 23.3 | |
| F (%) | 50.8 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice (n = 9)[1]
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Dosage:4 mg/kg (IV), 20 mg/kg (IP)
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Administration:IV, IP, once (Pharmacokinetic Analysis)
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Result:Exhibited desirable pharmacokinetic properties.
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Animal Model:BALB/c nude mice (5-6 weeks, HCT116 xenograft model)[1]
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Dosage:0, 25, 50 and 100 mg/kg
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Administration:IP, once daily for 21 days
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Result:Significantly inhibited the tumor growth, the tumor growth inhibitions were 28%, 40% and 44% at doses of 25, 50 and 100 mg/kg, respectively.
Chemical Information
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CAS No. 2418559-01-8
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Molecular Weight 483.95
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Formula C26H22ClN7O
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SMILES
O=C(NC1=CC=CC=C1N)C2=CC=C(CN3C=NC4=C(NC5=CC=C(C)C=C5)N=C(Cl)N=C34)C=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)
HDAC1/2 and CDK2-IN-1 Related Classifications
HY-143497 Related Classifications
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