HDAC8-IN-17
HDAC8-IN-17 is a histone deacetylase 8 inhibitor with human IC50 values of 0.08 μM, 0.44 μM, and 1.9 μM, and high selectivity over HDAC1, HDAC2, HDAC3, and HDAC6. HDAC8-IN-17 exhibits slow-binding, reversible uncompetitive inhibition via allosteric binding to the enzyme-substrate complex. HDAC8-IN-17 induces selective hyperacetylation of SMC3. HDAC8-IN-17 can be used for the research of cancer.
For research use only. We do not sell to patients.
- Formula: C23H16F3N3O4S
- Molecular Weight:487.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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HDAC1 5.8 μM (IC50) |
HDAC2 8.3 μM (IC50) |
HDAC3 29 μM (IC50) |
HDAC8 0.08 μM (IC50) |
In Vitro
HDAC8-IN-17 (compound 3r) (0-30 min) potently and time-dependently inhibits recombinant human HDAC8 enzyme, with an IC50 of 0.08 μM after 30 min of pre-incubation[1].
HDAC8-IN-17 (30 min) exhibits significantly higher selectivity for recombinant human HDAC8 than for HDAC1, HDAC2, HDAC3, and HDAC6; for HDAC1, the most potently inhibited off-target subtype, the selectivity reaches at least 72.5-fold[1].
HDAC8-IN-17 (44.44-225 nM; 30 min) is a reversible non-competitive inhibitor of recombinant human HDAC8, which preferentially binds to the enzyme-substrate complex[1].
HDAC8-IN-17 does not inhibit trypsin, confirming that its observed inhibitory activity is specific to HDAC8[1].
HDAC8-IN-17 (0.4-11 μM; 24 h) selectively induces hyperacetylation of SMC3 in THP-1 cells, confirming its functional inhibitory effect on HDAC8 in a cellular context[1].
HDAC8-IN-17 (72 h) inhibits the viability of human cancer cell lines Jurkat, THP-1, A549 and HCT116, with the strongest potency against THP-1 cells (GI50 = 9 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 human leukemia cells
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Concentration:0.4 μM, 1.2 μM, 3.7 μM, 11 μM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in acetylated SMC3 levels, with significant hyperacetylation observed at 3.7 μM and 11 μM compared to DMSO-treated controls.
Caused no significant increase in acetylated Histone H3 or α-tubulin levels at any tested concentration.
Chemical Information
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Molecular Weight 487.45
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Formula C23H16F3N3O4S
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SMILES
O=C(C(N1CC2=CC=C(C(F)(F)F)C=C2)=C(/C=C(C(N3)=O)/C(NC3=S)=O)C4=C1C=CC=C4)OC
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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)
HDAC8-IN-17 Related Classifications
HY-187382 Related Classifications
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