1,7-bis-boc-1,4,7-triazaheptane

1,7-Bis-Boc-1,4,7-triazaheptane is an alkyl ether-based PROTAC linker used for synthesizing PROTACs [1].

Propynol Ethoxylate is a PEG-based linker for PROTACs [Proteolysis Targeting Chimeras] that connects two essential ligands, facilitating the formation of PROTAC molecules and enabling selective protein degradation via the ubiquitin-proteasome system within cells.

XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1, with a DC50 of 19 nM, used for researching MYC-driven castration-resistant prostate cancer (CRPC). It effectively inhibits the growth of 22Rv1 cells (IC50 = 7 nM) and exhibits antitumor efficacy in vivo. XYD049 downregulates CRPC-associated oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 comprises a molecular glue linker (black part) NH2-C5-NH-Boc, a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride, and a target protein ligand (red part) GSPT1 ligand-1, with the E3 ligase ligand + linker forming the conjugate E3 Ligase Ligand-linker Conjugate 158.

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.

DNA Crosslinker 4 (dihydrochloride) is a potent binder of the DNA minor groove with inhibitory effects on cancer cell lines NCI-H460, A2780, and MCF-7. It is utilized in research for anticancer applications [1].