at-6

AT6 is a PROTAC AT1 analog which is a highly selective bromodomain (Brd4) degrader.

SD-436 is a selective and highly efficient STAT3 PROTAC degrader (DC50 = 0.5 μM), with an IC50 of 19 nM for STAT3, significantly higher than for STAT1/4/5/6. SD-436 depletes STAT3 and induces tumour regression in mouse leukaemia and lymphoma xenograft models.

YT 6-2 is an autophagy-targeting ligand (ATL) aimed at p62/SQSTM1, used in the synthesis of AUTOTAC degrader ATC-324. ATC-324 induces the formation of AR/p62 complexes, leading to the autophagic-lysosomal degradation of AR. It reduces nuclear AR levels, downregulates the expression of AR and AR-v7 target genes, and also degrades common AR mutants in PCa.

YT 6-2 analog-1 (compound 2-3) serves as an autophagy-targeting ligand (ATL) aimed at p62/SQSTM1, useful in synthesizing the AUTOTAC degrader ATC-324 for the Androgen Receptor (AR). ATC-324 promotes the formation of AR/p62 complexes, leading to the autophagic-lysosomal degradation of AR. It effectively reduces nuclear AR levels, downregulates the expression of AR and AR-v7 target genes, and can degrade common AR mutants found in prostate cancer (PCa).

Alkyne-PEG6-acid is a bifunctional PEG crosslinker utilized in biological conjugation and as a component in small molecule synthesis. This crosslinker bears a carboxyl group at one end and an alkyne group at the other. In PROTACs, it is known as 2-2-2-2-2-2-6 PROTAC® linker and is also employed in the synthesis of antibody-drug conjugates.

PROTACc-Met degrader-6 is a potent and orally active c-Met PROTAC degrader. It effectively promotes the degradation of c-Met protein, with DC50 values of 0.52 nM in EBC-1 cells and 0.45 nM in Hs746T cells. This compound almost completely abolishes the migration and invasion capabilities of tumor cells, significantly induces apoptosis (apoptosis), and arrests the cell cycle at the G0/G1 phase. PROTACc-Met degrader-6 is useful for studying various cancers, including non-small cell lung cancer and gastric cancer.

HEMTAC CDK4/6 degrader 1 is a PROTAC connected by ligands for HSP90 and CDK4/6 with a \( K_d \) value of 35.7 μM. It induces CDK4/6 degradation in B16F10 melanoma cells, arrests the cell cycle at the G0/G1 phase, and induces apoptosis. HEMTAC CDK4/6 degrader 1 can be used in cancer research [1].