| Name | dBET6 |
| Description | dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity. |
| Animal Research | MOLT4 human T-ALL cells are intravenously injected into NSG mice (2×106 cells/mouse). Luminescence is utilized to monitor engraftment (evident at day 6), at which point mice are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 8), JQ1 (20 mg/kg QD, n = 9) or vehicle (captisol, n = 9) treatment for 14 days. Survival of all three cohorts is subsequently monitored using hind limb paralysis caused by a high femoral leukemic burden as a defined endpoint. SUPT11 human T-ALL cells (mCherry+ and Luciferase+) are intravenously injected into NSG mice (2.52×106 cells/mouse). Luminescence is used to monitor successful engraftment, occurring 10 days after injection. At this point, animals are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 7), JQ1 (7.5 mg/kg BID, n = 7) or vehicle (captisol, n = 7) treatment for 18 days. Treatment burden is assessed via total body luminescence imaging as well as by bone marrow infiltration by mCherry+ T-ALL cells. |
| In vitro | dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4. |
| In vivo | dBET6 (7.5 mg/kg, p.o., BID) reduces leukemic burden in a disseminated mouse model of T-ALL. |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 10 mM
|
| Keywords | dBET-6 | Apoptosis | PROTACs | Inhibitor | inhibit | dBET6 | Epigenetic Reader Domain | dBET 6 |
| Inhibitors Related | Stavudine | Sodium 4-phenylbutyrate | Tributyrin |
| Related Compound Libraries | Bioactive Compound Library | Epigenetics Compound Library | Glutamine Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-COVID-19 Compound Library | Anti-Cancer Active Compound Library |
United States
