CPI-637

Catalog No.S8190 Batch:S819002

Technical Data

Formula	C₂₂H₂₂N₆O
Molecular Weight	386.45	CAS No.	1884712-47-3
Solubility (25°C)*	In vitro	DMSO	26 mg/mL (67.27 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
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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