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].
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- CAS. Nr.: 1613310-15-8
- Formel: C16H14O2
- Molecular Weight:238.28
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
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.
Chemical Information
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CAS. Nr. 1613310-15-8
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Molecular Weight 238.28
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Formel C16H14O2
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SMILES
O=C(C1=CC=CC=C1)/C=C(C2=CC=CC=C2)\CO
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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)