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PROTAC BRD2/BRD4 degrader-1

CAS No. :

MCE 站：PROTAC BRD2/BRD4 degrader-1

产品活性：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。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。

研究领域：Epigenetics  |  PROTAC

作用靶点：Epigenetic Reader Domain  |  PROTAC ａnd Building Blocks

In Vitro: PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, ａnd the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells.
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, ａnd the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells.
PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines.
PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI₅₀ values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells.
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).

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