composition

tert-Butyl 11-aminoundecanoate 是一种属于 PEG 类的 PROTAC linker。它可用于合成一系列 PROTAC 分子。

Br-C10-methyl ester 是一种属于 alkyl/ether 类的 PROTAC linker，可用于一系列 PROTAC 分子的合成。PROTAC 分子含有两个通过 linker 连接的不同配体，一种是 VHL 配体部分，另一种是靶蛋白配体。

Monoethyl pimelate 是一种属于 alkyl/ether 类的 PROTAC linker 可用于特异性的 BCL-XLPROTAC 降解剂 (S,R,S)-AHPC-Me-C7 ester 的合成。

Tos-PEG4-t-butyl ester (Tos-PEG4-Boc) is a PROTAC linker characterized by its PEG composition. This compound plays a crucial role in the synthesis of a range of PROTACs, including BI-3663, a highly selective PTK2/FAK PROTAC. It employs cereblon ligands to target E3 ligases for the degradation of PTK2, exhibiting potent inhibitory activity with an IC50 of 18 nM[1].

Boc-Pip-alkyne-Ph-COOH, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in synthesizing PROTACs including ARD-266. This compound demonstrates significant efficacy in promoting the degradation of androgen receptor (AR) protein across AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, showcasing DC50 values ranging from 0.2-1 nM[1].

NH2-PEG5-C6-Cl (K-7) is a PROTAC linker characterized by its PEG composition. It can be utilized in the synthesis of various PROTACs, facilitating the degradation of intracellular molecules via autophagy[1].

Phthalimide-PEG4-MPDM-OH, a PROTAC linker with a PEGs composition, has applications in the synthesis of various PROTACs. These PROTACs consist of a linker connecting two distinct ligands: one binds to an E3 ubiquitin ligase, while the other binds to the target protein. By leveraging the intracellular ubiquitin-proteasome system, PROTACs selectively induce the degradation of target proteins [1].

S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate, an ADC linker, is a glutathione cleavable compound used for the attachment of monoclonal antibodies (mAb) in antibody-drug conjugates (ADCs). It specifically refers to the Alkyl-Chain composition of the linker portion of these molecules [1].

DZ-837 是一种特定针对BCL6的PROTAC分子。其结构包括BCL6 ligand-2 作为PROTAC靶蛋白配体，E3 泛素连接酶配体 Thalidomide-4-OH，以及连接这两者的 PROTAC Linker。E3 泛素连接酶配体和 Linker 结合形成的化学结构为 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione。

JMV7048是一种针对PXR(Pregnane X 受体)的高效PROTAC降解剂,具有379 nM的DC50值.该化合物通过连接E3 CRBN泛素连接酶和26S蛋白酶体,促使PXR蛋白发生多泛素化并进行降解.JMV7048能够通过降低结肠癌干细胞中的PXR蛋白表达,显著增强这些细胞对化疗药物的敏感性,进而有效延缓体内的癌症复发.此化合物由PXR激动剂JMV6944、linker以及Thalidomide 5-fluoride组成.