DNA/RNA Synthesis Degrader

aTAG 4531 (CFT-4531) is a PROTAC-class degrader that induces the degradation of the MTH1/aTAG fusion protein by recruiting cereblon, with a DC₅₀ of 0.28 nM in Jurkat cells. aTAG 4531 inhibits MTH1 enzymatic activity, with a K_i of 1.8 nM. aTAG 4531 rapidly, selectively and reversibly regulates SMART-CAR protein levels, CAR-mediated target cell killing and IL-2 release, and is applicable both in vitro and in vivo. aTAG 4531 can be used in studies of targeted protein degradation, target validation and CAR-T activity regulation.

And1 degrader 1 (Compound A15) is a degrader of the acidic nucleoplasmic DNA-binding protein 1 (And1), which can significantly induce the degradation of And1 in NSCLC cells. And1 degrader 1 (5 μM) combined with Olaparib (HY-10162) (1 μM) effectively inhibits the proliferation of A549 and H460 cells. And1 degrader 1 can be used in cancer research.

WRN inhibitor 20 (Compound 14c) is a WRN degradation agent. WRN inhibitor 20 exhibits strong degradation activity in various cells, such as HCT-116 (DC₅₀ = 1.7 µM), SW-48 (DC₅₀ = 3.0 µM), and SW-480 (DC₅₀ = 5.9 µM) cells. WRN inhibitor 20 exhibits potent anti proliferative, pro apoptotic, migration inhibiting, and DNA damage inducing effects in MSI-H cells. WRN inhibitor 20 can be used for research on cancer.

Anticancer agent 355 is a highly selective and potent anticancer agent, with IC₅₀ values of 64.66 μM and 13.35 μM against HeLa and MDA-MB-231 cancer cells, respectively. Anticancer agent 355 induces plasmid DNA degradation via intercalation or minor groove binding, and disrupts the tertiary structure of BSA by interfering with the interactions of amino acid side chains. Anticancer agent 355 can be used in the research of cervical cancer and breast cancer.