HDAC8-IN-16
HDAC8-IN-16 is a selective histone deacetylase 8 (HDAC8) inhibitor with an IC50 of 0.16 μM. HDAC8-IN-16 induces cell apoptosis, triggers G2/M phase cell cycle arrest, and moderately inhibits cancer cell proliferation. HDAC8-IN-16 is applicable to relevant research on colorectal cancer.
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- CAS. Nr.: 2464465-06-1
- Formel: C21H24N4O3
- Molecular Weight:380.44
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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HDAC8 0.16 μM (IC50) |
HDAC8-IN-16 (Compound 16) (48 h) exhibits moderate antiproliferative activity against Jurkat, MOLT-4 and HCT116 tumor cells, with the strongest activity against HCT116 cells (IC50 = 16.12 μM), while it shows only weak or no activity against K562, HL-60 and HeLa cells[1].
HDAC8-IN-16 (5-20 μM; 48 h) significantly increases the acetylation level of SMC3, a specific substrate of HDAC8, in HCT116 cells, confirming that it inhibits HDAC8 at the cellular level[1].
HDAC8-IN-16 (5-20 μM; 48 h) induces dose-dependent apoptosis in HCT116 cells[1].
HDAC8-IN-16 (5-20 μM; 48 h) arrests HCT116 cells at the G2/M phase of the cell cycle in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h
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Result:Had a marginal effect on Ac-SMC3 levels at 5 μM and 10 μM.
Induced a significant, noticeable accumulation of Ac-SMC3 at 20 μM.
Had no significant effect on Ac-α-tubulin or histone H3 acetylation levels.
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Cell Line:HCT116 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h (treatment); 15 min (staining incubation at room temperature)
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Result:Increased early apoptosis from 1.87% to 2.81% and late apoptosis from 0.90% to 3.12% at 5 μM.
Increased early apoptosis to 17.37% and late apoptosis to 7.53% at 10 μM.
Increased early apoptosis to 17.37% and late apoptosis to 25.57% at 20 μM, showing a dose-dependent increase in apoptotic cells.
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Cell Line:HCT116 cells
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Concentration:5 μM, 10 μM, 20 μM
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Incubation Time:48 h (treatment); overnight (fixation at 4 °C); 30 min (staining incubation at room temperature)
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Result:Decreased G0/G1 phase from 67.23% to 57.84%, increased S phase from 16.87% to 19.01%, and increased G2/M phase from 15.90% to 23.15% at 5 μM.
Decreased G0/G1 phase to 40.67%, increased S phase to 27.13%, and increased G2/M phase to 32.20% at 10 μM.
Decreased G0/G1 phase to 27.62%, increased S phase to 27.02%, and increased G2/M phase to 45.36% at 20 μM, showing a pronounced G2/M phase arrest.
Chemical Information
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CAS. Nr. 2464465-06-1
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Molecular Weight 380.44
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Formel C21H24N4O3
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SMILES
O=C(N1CCC(CC1)[C@H](CO)O)C2=NN(C3=C2C=CC=N3)CC4=CC=CC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
HDAC8-IN-16 Related Classifications
HY-182035 Related Classifications
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