nh2-c5-nh-boc

NH2-C5-NH-Boc (PROTAC Linker 23) is an alkyl chain-based PROTAC linker used in the synthesis of PROTACs.

NH2-C2-amido-C2-Boc is an alkyl ether-based PROTAC linker used in synthesizing various PROTACs, including PROTAC CDK2 9 Degrader-1[1]. NH2-C5-NH-Boc also serves as a suitable precursor for synthesizing these PROTACs.

XD2-149 is a PROTAC compound designed to target STAT3. It is composed of the PROTAC target protein ligand Napabucasin, the E3 ligase Thalidomide, and the linker NH2-C5-Azacyclohexane-N-Boc. The conjugate of the E3 ligase and linker is Thalidomide-NH-C5-azacyclohexane-N-Boc, with Thalidomideacid serving as the active comparator for the target protein ligand.

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.