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CPI-203 is a potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM. CPI-203 inhibits BRD4 in vitro and in cells, but it does not affect BRD4 kinase activity in vitro. 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. CPI-203 arrests the growth of leukemic T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice. In contrast, in vivo, specific Ser2 phosphorylation by either endogenous BRD4 or exogenous BRD4 FEE-AAA was markedly decreased by treatment with the inhibitor.
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Source | Genes Dev (2015). Figure 6. CPI-203 |
| Method | qRT–PCR | |
| Cell Lines | LSK CD150+ CD48− HSCs | |
| Concentrations | 0.5 μM | |
| Incubation Time | 24 h | |
| Results | As expected, MycmRNAwas reduced by twofold to threefold compared with mock-treated HSCs in both groups, while there was no difference in Myc expression between the Erg+/− and Erg+/+ groups |
| Cell Experiment | |
|---|---|
| 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) |
| Preparation method | Incubating MCL primary cells and cell lines as indicated with lenalidomide and/or CPI203. Adding MTT for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Using untreated control cells to represent values . The GI50 is calculated as the concentration that produced 50 % growth inhibition. Using the Calcusyn software version 2.0 to calculate Combination indexes (CIs) . When CI <1 ,the interaction between two drugs is considered synergistic. |
| Concentrations | 10 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | REC-1 tumor-bearing mice |
| Formulation | |
| Dosages | 2.5 mg/kg twice daily |
| Administration | i.p |
| Molecular Weight | 399.9 |
| Formula | C19H18ClN5OS |
| CAS Number | 1446144-04-2 |
| Solubility (25°C) | DMSO ≥ 40 mg/mL (warmed) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Epigenetic Reader Domain Products |
|---|
| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
| I-BET151
I-BET151 (GSK1210151A) is an inhibitor of the BET family with IC50 of 0.5 μM, 0.25 μM and 0.79 μM for BRD2, BRD3 and BRD4, respectively. |
| (+)-JQ1
(+)-JQ1 is a BET bromodomain inhibitor that acts on BRD4(2) with an IC50 of 33 nM and binds to all bromodomain domains in the BET family, but not to bromodomain domains outside the BET family. JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway, and JQ1 down-regulates CD47 expression through a C-MYC-mediated pathway. |
| I-BET-762
I-BET-762 (GSK525762) is a selective small molecule BET inhibitor. |
| CPI-0610
CPI-0610 is a novel BET protein bromodomain inhibitor. |
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