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BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc in HT-29 cells. BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase. BRD4 Inhibitor-20 (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie.
| Molecular Weight | 358.41 |
| Formula | C18H18N2O4S |
| CAS Number | 2490311-14-1 |
| Solubility (25°C) | DMSO 95 mg/mL |
| Storage | 4°C, protect from light |
| Related Epigenetic Reader Domain Products |
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| 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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