protac brd4 degrader-2

PROTAC BRD4 Degrader-2 is an efficacious degrader of PROTAC BRD4(BRD4 BD1,IC50 of 14.2 nM).

PROTAC BRD4 Degrader-29 (compound 7a) 是一种有效的BRD4 PROTACs降解剂，DC50为89.4 nM，在癌症研究中具有重要作用。

PROTAC BRD4 Degrader-28 (Compound 4) 是一种针对BRD4的PROTAC降解剂，并有潜力应用于癌症研究。

PROTACBRD4 Degrader-21 (Comp 74)为BRD4降解剂，其在小鼠荷瘤异种移植模型中展现出显著抑制肿瘤生长的能力，适用于抗癌研究。

PROTACBRD4Degrader-22 (Compd 44h) 作为BRD4PROTAC降解剂，展现出高效性，其在MOLT4细胞中24小时处理后的pDC50值达到9.2。

PROTACBRD4 Degrader-20 (compound 195) 作为一种双功能化合物，同时具有BRD4降解剂的功能。

PROTACBRD4 Degrader-25 (Compound 1-f) 作为一种有效的BRD4降解剂，主要应用于癌症及其他与溴结构域相关的疾病研究领域。

PROTAC BRD4 Degrader-27 是一种精准针对BRD4的PROTAC，不影响BRD2 BRD3。此化合物包含E3 泛素酶配体Thalidomide-4-OH、连接体PROTAC Linkerγ-Aminobutyric acid以及针对BRD4的PROTAC 靶蛋白配体PROTAC BRD4 ligand-3，后者的参考活性物质为Mivebresib。此外，E3 泛素酶配体与Linker的结合产物是Pomalidomide 4'-alkylC3-acid。

ARV-771 是基于 PROTAC 技术的有效 BET 降解剂，对 BRD2(1)、BRD2(2)、BRD3(1)、BRD3(2)、BRD4 (1) 和 BRD4(2)的 Kd 分别为 34、4.7、8.3、7.6、9.6 和 7.6 nM。

Lenalidomide-PEG1-azide is an E3 ligase ligand-linker conjugate that incorporates the cereblon ligand based on Lenalidomide and a linker. It is designed for use in the development of PROTAC BRD4 Degrader-2[1].

PROTAC BRD2 BRD4 degrader-1 (compound 15) serves as a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination of BRD4 and BRD2 compared to BRD3. Its efficacy in suppressing solid tumors manifest with minimal cytotoxic effects. This compound comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN) cullin 4A[1].

PROTAC BRD4 Degrader-8 is a potent BRD4 inhibitor, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells[1]. PROTAC BRD4 Degrader-8 (compound 8; 6 days) inhibits the proliferation of PC3 prostate cancer cells, with an IC50 of 28 nM[1].PROTAC BRD4 Degrader-8 (4 h) suppresses MYC gene transcript in MV4-11 AML cells, with an IC50 of 11 nM[1].PROTAC BRD4 Degrader-8 (4 h) potently degrades the BRD4 protein in PC3 prostate cancer cells, with an DC50 of 7.5 nM[1]. [1]. Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607.

PROTACBRD3 BRD4-L degrader-2 是一款可以特异性地降解BRD3和BRD4-L的PROTAC分子，其对BRD3的Ki值为16.91 nM，对BRD4-L为2.8 nM。在小鼠异种移植模型中，该分子展示了卓越的抗肿瘤效果，可被应用于癌症相关研究。

PROTAC BRD4 Degrader-5-CO-PEG3-N3 (Compound 2) 是一款专为 PAC 设计的PROTAC-linker偶联物,采用了含有BRD4降解剂GNE-987的构造,并通过3个PEG的linker进行连接.该化合物也是一种效率高的点击化学试剂,内含Azide基团,可通过铜催化的叠氮-炔环加成反应(CuAAc)与含Alkyne基团的分子反应.此外,它还能通过与含DBCO或BCN基团的分子进行菌株促进的炔-叠氮环加成反应(SPAAC)进行反应.