protac brd4 degrader-5

PROTAC BRD4 Degrader-5 是一种可有效降解 HER2 阳性和阴性乳腺癌细胞系中的 BRD4 的 PROTAC， 由von Hippel-Lindau配体和BRD4配体相连形成。

cBu-Cit-PROTAC BRD4 Degrader-5，一种与cBu-Cit偶联的PROTAC降解剂，能够有效地降解HER2阳性及阴性乳腺癌细胞系中的BRD4。

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.

PROTAC BRD4 degrader for PAC-1 (compound 5) is a chimeric BET degrader GNE-987 conjugated with a disulfide-containing linker[1]. This PROTAC-linker conjugate specifically targets and degrades BRD4, enabling selective proteolysis of PAC-1.

dBRD9 HCl 是一种PROTAC，包含cereblon E3连接酶配体与BRD9抑制剂BI 7273。dBRD9 HCl 是有效和选择性的BRD9降解剂，在MOLM-13细胞中IC50的为56.6nM。dBRD9 HCl 在浓度高达5μM 时不会降解BRD4或BRD7。dBRD9 HCl 在人AML 细胞系中显示出抗增殖作用。

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.

(S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 is a synthetic E3 ligase ligand-linker conjugate comprised of a VHL ligand and a linker. It is utilized in PROTAC BRD4 Degrader-5 and PROTAC BRD4 Degrader-5-CO-PEG3-N3.