CPI637 是一种选择性和细胞活性的苯二氮卓 CBP/EP300 溴结构域抑制剂，其对CBP、EP300和BRD4 BD-1的IC50值分别为 0.03、0.051 和 11.0 μM，对CBP的EC50值为 0.3 μM。

CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.

CPI-637 inhibits MYC expression in AMO-1 cells (EC50=0.60 μM)[1].

Ki Determination: Inhibition of human full-length recombinant PARP-1 by [32P]NAD+ incorporation is measured. The [32P]ADP-ribose incorporated into acid insoluble material is quantified using a PhosphorImager. Ki is calculated by nonlinear regression analysis.

AMO-1 cells (DSMZ) were plated at 20,000 cells/well in 96-well plates in Iscove's Modified Dulbecco's Medium supplemented with 10% fetal calf serum. Cells were treated for 6 h with a dose titration of CPI-637 starting from a 5 μM top concentration. After 6 h, cells were lysed and processed for QuantiGene Plex expression analysis and data were collected on a MAGPIX multiplex Luminex instrument.(Only for Reference)

1884712-47-3

C22H22N6O

386.459

CPI 637

H2O:<1 mgml
Ethanol:<1 mgml
DMSO:26 mg/mL (67.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years