Home Epigenetics Epigenetic Reader Domain inhibitor - Histone Acetyltransferase inhibitor CPI-637 For research use only.

CPI-637

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

CPI-637 Chemical Structure

CAS No. 1884712-47-3

Purity & Quality Control

CPI-637 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

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

Chemical Information & Solubility

Molecular Weight 386.45 Formula

C22H22N6O
CAS No. 1884712-47-3 SDF Download CPI-637 SDF
Smiles CC1CC(=O)NC2=CC=CC(=C2N1)C3=CC4=C(C=C3)N(N=C4C5=CN(N=C5)C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 26 mg/mL ( (67.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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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