HDAC8-IN-14
HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia.
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- Formule: C37H27Cl2N5O
- Masse moléculaire:628.55
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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HDAC8 9 nM (Ki) |
Caspase-3 |
HDAC8-IN-14 (Compound 5e) (0.1-100 μM, 48 h) exhibits a low IC50 value of 90 nM in MOLT-4 cells, along with IC50 values of 1.98 μM in EL-4, 1.17 μM in YAC-1, and 18.94 μM in L1210 cells, while demonstrating a significantly higher IC50 of 39.20 μM in the non-cancerous HEK-293 cell line, indicating its selectivity and safety toward non-cancerous cells at effective concentrations[1].
HDAC8-IN-14 (100 nM, 30 min) shows significant ROS induction as measured by the fluorescent dye H2DCFDA (HY-D0940) in MOLT-4 cells[1].
HDAC8-IN-14 (48 h) induces mitochondrial depolarization, evidenced by a shift in JC-1 fluorescence, triggers both apoptosis (~ 10 %) and necrosis (~ 30 %), and causes cell cycle arrest characterized by a 20 % increase in the sub-G0 apoptotic population alongside a reduction in G0/G1 and G2/M phases and a slight S-phase accumulation[1].
HDAC8-IN-14 (50-100 nM, 48 h) induces a significant upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered, indicating that it activates the intrinsic apoptotic pathway through a Bcl-2-independent mechanism in MOLT-4 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4 cells
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Concentration:50 nM, 100 nM
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Incubation Time:48 h
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Result:Induced a significant upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The left thigh of each female Swiss albino mice (6-8 weeks) was injected with 0.5 million DLA cells to induce a tumor[1].
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Dosage:50 mg/kg
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Administration:I.p., once daily for 30 days
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Result:Reduced tumor burden compared to the control group.
Resulted in the upregulation of cytochrome c, cleaved caspase 3, and proapoptotic Bax, the levels of the anti-apoptotic Bcl-2 remained unchanged.
Exhibited reduced nuclear density, suggesting decreased tumor cell proliferation.
No significant histopathological alterations were observed in the liver and kidney tissues of treated mice.
Indicated no toxicity to liver function.
The body weight of the animals at the end of the study showed no variation.
Chemical Information
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Masse moléculaire 628.55
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Formule C37H27Cl2N5O
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SMILES
O=C1/C(CNC/C1=C\C2=CN(C3=CC=CC=C3)N=C2C4=CC=C(Cl)C=C4)=C/C5=CN(C6=CC=CC=C6)N=C5C7=CC=C(Cl)C=C7
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC8-IN-14 Related Classifications
HY-178380 Related Classifications
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