C646

• 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.

• 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 .

• CAS Number :

  328968-36-1

• 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