CPI-637

Catalog No.S8190

For research use only.

CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.

CPI-637 Chemical Structure

CAS No. 1884712-47-3

Selleck's CPI-637 has been cited by 1 Publication

Purity & Quality Control

Choose Selective Epigenetic Reader Domain Inhibitors

Biological Activity

Description CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.
Targets
CBP [1]
(Cell-free assay)
EP300 [1]
(Cell-free assay)
0.03 μM 0.051 μM
In vitro

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

Protocol (from reference)

Cell Research:[1]
  • Cell lines: AMO-1 cells
  • Concentrations: 0-5 μM
  • Incubation Time: 6 h
  • Method: 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 386.45
Formula

C22H22N6O

CAS No. 1884712-47-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CC(=O)NC2=CC=CC(=C2N1)C3=CC4=C(C=C3)N(N=C4C5=CN(N=C5)C)C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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