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Background: C646 binds to p300 as the Z-isomer forming hydrogen bonds between Thr1411, tYR1467, Trp1466 and Arg1410 on the side chains of p300 and oxygen atoms of C646. C646 is also capable of inhibiting a variety of p300 HAT mutants, including T1411A, Y1467F, W1466F and R1410A with IC50 values of 3.4 µM, 7 µM, 5 µM and 2.5 µM respectively.
CAS Number: 328968-36-1
Description: C646, a pyrazolone-containing small molecule, is a cell-permeable histone acetyltransferase (HAT) inhibitor that competitively and selectively inhibits the HAT activity of p300, a transcriptional co-activator involved in a variety of gene regulatory pathways and protein acetylation events, with the Ki value of 400 nM and an IC50 value of 1.6 µM .
Solubility: Soluble in DMSO
Storage Stability: Store at or below -20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.
Target: p300
Biosafety Level: Not applicable (BSL-1)
References: Bowers EM, et al. Chem Biol. 2010 May 28;17(5):471-82.