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dBET1 treatment down regulates MYC and PIM1 transcription. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50= 0.14 μM, compare to IC50= 1.1 μM with JQ1).
In vivo, administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors.
| Cell Experiment | |
|---|---|
| Cell lines | LS174t cells |
| Preparation method | To determine colony formation ability, cells (1-2x10^3) were plated on six well plates. After 48 h, cells were treated with the indicated concentrations of JQ1, dBET1 or MZ1 for 3–5 days. Cells were fixed with methanol and stained with crystal violet. |
| Concentrations | 0,100,1000 nM |
| Incubation time | 3–5 days |
| Animal Experiment | |
|---|---|
| Animal models | Aged male mice (C57BL/6N, 18–20 months) |
| Formulation | vehicle (40% Captisolin MilliQ water), 1, 10, or 30 mg/kg dBET1 further diluted in 300 μL 0.9% saline |
| Dosages | 1, 10, or 30 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 785.27 |
| Formula | C38H37ClN8O7S |
| CAS Number | 1799711-21-9 |
| Solubility (25°C) | DMSO 40 mg/mL |
| 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 |
|---|
| 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. |
| RVX-208
Apabetalone (RVX-208) is a first-in-class, small molecule inhibitor of BET bromodomain with IC50 of 0.51 μM for BD2. |
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