CPI-637

Catalog No.S8190 Batch:S819001

Technical Data

Formula	C₂₂H₂₂N₆O
Molecular Weight	386.45	CAS No.	1884712-47-3
Solubility (25°C)*	In vitro	DMSO	27 mg/mL (69.86 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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.

Cell Assay:^{^[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.

References

[1] Taylor AM, et al. ACS Med Chem Lett. 2016, 7(5):531-6.

Selleck's CPI-637 has been cited by 2 publications

P300 Interacted With N-Myc and Regulated Its Protein Stability via Altering Its Post-Translational Modifications in Neuroblastoma [ Mol Cell Proteomics, 2023, 22(3):100504]	PubMed: 36708875
Y08197 is a novel and selective CBP/EP300 bromodomain inhibitor for the treatment of prostate cancer. [ Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0237-5]	PubMed: 31097763

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SHIPPING AND STORAGE
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