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CPI-203

Catalog No. T6026   CAS 1446144-04-2
Synonyms: CPI 203, CPI203

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

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CPI-203 Chemical Structure
CPI-203, CAS 1446144-04-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 60.00
5 mg In stock $ 108.00
10 mg In stock $ 172.00
25 mg In stock $ 369.00
50 mg In stock $ 554.00
1 mL * 10 mM (in DMSO) In stock $ 94.00
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Purity: 99.66%
Purity: 99.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
Targets&IC50 BRD4:37 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.
Synonyms CPI 203, CPI203
Molecular Weight 399.9
Formula C19H18ClN5OS
CAS No. 1446144-04-2

Storage

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

Solubility Information

DMSO: 72 mg/mL(180 mM)

TargetMolReferences and Literature

1. Devaiah BN, et al. Proc Natl Acad Sci U S A. 2012, 109(18), 6927-6932.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Inhibitor Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library Bioactive Compound Library Kinase Inhibitor Library Chromatin Modification Compound Library Apoptosis Compound Library PPI Inhibitor Library Histone Modification Compound Library

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Keywords

CPI-203 1446144-04-2 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain Inhibitor inhibit CPI 203 CPI203 inhibitor

 

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