β-Hydroxymethyl chalcone
β-Hydroxymethyl chalcone is a time-dependent selective HDAC2 inhibitor, with IC50 values of 0.17 μM (24 h) and 9.19 μM (1 h). After binding to the catalytic zinc ion in the active pocket of HDAC2, β-Hydroxymethyl chalcone undergoes an intramolecular nucleophilic attack to form a cyclic product, resulting in time-dependent tight binding. β-Hydroxymethyl chalcone can be used for the study of HDAC2 selective inhibition and related epigenetic targets[1].
For research use only. We do not sell to patients.
- CAS No.: 1613310-15-8
- Formula: C16H14O2
- Molecular Weight:238.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
hHDAC2 0.17 μM (IC50, 24 h) |
hHDAC2 9.19 μM (IC50, 1 h) |
hHDAC1 2.74 μM (IC50, 24 h) |
hHDAC1 3.68 μM (IC50, 1 h) |
hHDAC3 ~ 50 μM (IC50, 1h, 24 h) |
In Vitro
β-Hydroxymethyl chalcone (1-24 h) exhibits time-dependent selective inhibition of HDAC2 in in vitro recombinant enzymatic assays. The IC50 values after 1 h and 24 h of incubation are 9.19 μM and 0.17 μM, respectively, with an approximately 20-fold selectivity for HDAC2 over HDAC1 (3.68 μM at 1 h; 2.74 μM at 24 h), and shows weak activity against HDAC3 (approximately 50 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1613310-15-8
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Molecular Weight 238.28
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Formula C16H14O2
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SMILES
O=C(C1=CC=CC=C1)/C=C(C2=CC=CC=C2)\CO
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)