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CPI203

Catalog No. T2442   CAS 202591-23-9
Synonyms: CPI 203, CPI-203

CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).

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CPI203 Chemical Structure
CPI203, CAS 202591-23-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 50.00
10 mg In stock $ 75.00
25 mg In stock $ 120.00
50 mg In stock $ 221.00
100 mg In stock $ 398.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.71%
Purity: 99.13%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CPI203 (CPI 203) is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
Targets&IC50 BET bromodomain:37 nM
In vitro CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. [1] CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. [2]
Kinase Assay BRD4 α-screen assay: The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor.
Cell Research MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI <1. (Only for Reference)
Synonyms CPI 203, CPI-203
Molecular Weight 399.9
Formula C19H18ClN5OS
CAS No. 202591-23-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 200 mM

TargetMolReferences and Literature

1. Devaiah BN, et al. Proc Natl Acad Sci U S A. 2012, 109(18), 6927-6932. 2. Moros A, et al. Leukemia. 2014. doi: 10.1038/leu.2014.106.

Related compound libraries

This product is contained In the following compound libraries:
Epigenetics Compound Library Kinase Inhibitor Library

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Keywords

CPI203 202591-23-9 Chromatin/Epigenetic Epigenetic Reader Domain CPI 203 CPI-203 inhibitor inhibit

 

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