C646
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 .
Product Specifications
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.
Solubility
Soluble in DMSO
Molecular Formula
C24H19N3O6
Shipping Conditions
Room Temperature (continental US) or Gel Packs
Storage Conditions
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.
Calculated Molecular Weight
445.4 Da
CAS Number
328968-36-1
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