PROTAC BRD2/BRD4 degrader-1 (compound 15) 是一种高效、选择性的 BET 蛋白BRD4和BRD2降解剂，由Cereblon配体和BET配体相连。PROTAC BRD2/BRD4 degrader-1 快速诱导 BRD4 和 BRD2 的可逆、持久和选择性去除。它能够抑制肿瘤生长并具有低毒性。PROTAC BRD2/BRD4 degrader-1 由 BET 抑制剂、 linker 和 cereblon (CRBN)/cullin 4A 配体组成。
| 生物活性 | PROTACBRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET proteinBRD4andBRD2degrader, connected by ligands forCereblonandBET.PROTACBRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal ofBRD4andBRD2overBRD3. It effectively inhibits solid tumors with low cytotoxic effect.PROTACBRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide forcereblon(CRBN)/cullin 4A[1]. |
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体外研究
(In Vitro) | PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells[1].
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells[1].
PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines[1].
PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI50values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells[1].
PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC50: 0.081 μM), colon cancer (colo-205 IC50: 0.1557 μM) and thyroid cancer(TT IC50: 0.037451 μM)[1].
Cell Proliferation Assay[1] | Cell Line: | MV4-11 leukemia cells | | Concentration: | 100 nM | | Incubation Time: | ≥8 hours | | Result: | The BRD4 protein was reduced very efficiently. |
Western Blot Analysis[1] | Cell Line: | MV4-11 leukemia cells | | Concentration: | 10 , 50, 100, 500 nM | | Incubation Time: | 18 hours | | Result: | Performed depletion selectivity for BRD4 and BRD2 over BRD3, with good selectivity intra-BET proteins selectivity. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
