Home Epigenetics Epigenetic Reader Domain inhibitor CPI-203 For research use only.

CPI-203

CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.

CPI-203 Chemical Structure

CPI-203 Chemical Structure

CAS No. 1446144-04-2

Purity & Quality Control

CPI-203 Related Products

Signaling Pathway

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain Signaling Pathway

Biological Activity

Description CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
Targets
IL-6 [1]
(Cell-based assay)		 BRD4 [1]
(Cell-free assay)		 MYC [1]
(Cell-based assay)
30 nM 37 nM 99 nM
In vitro
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, CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells. [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 Cell lines 2 PBMC cultures from healthy donors and 9 MCL cell lines (Granta-519, JVM-2, UPN1, Z-138, JeKo-1, ZBR, JBR, Mino, REC-1 cells)
Concentrations 10 μM
Incubation Time 72 hours
Method

MCL primary cells and cell lines are incubated as indicated with 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.
In Vivo
In vivo

BRD4 mediates CTD Ser2 phosphorylation in vivo. [1] In REC-1 tumor-bearing mice, the combination of CPI203 (2.5 mg/kg i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis. [2]
Animal Research Animal Models REC-1 tumor-bearing mice
Dosages 2.5 mg/kg twice daily
Administration i.p

Chemical Information & Solubility

Molecular Weight 399.90 Formula

C19H18ClN5OS
CAS No. 1446144-04-2 SDF Download CPI-203 SDF
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)N)C4=CC=C(C=C4)Cl)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 79 mg/mL ( (197.54 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble


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In vivo
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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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