PRMT4 Degrader

MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC₅₀ of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC₅₀ of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )).

PROTAC CARM1 degrader-1 hydrochloride is a highly selective CARM1 PROTAC degrader, with a DC₅₀ of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 hydrochloride recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 hydrochloride downregulates the methylation level of CARM1 substrates in breast cancer cells, inhibits breast cancer cell migration, and exhibits no significant inhibitory effect on cell proliferation. PROTAC CARM1 degrader-1 hydrochloride is applicable for related research on breast cancer.

CM112 is a hydrophobic tag-based PRMT1 degrader (DC₅₀ = 0.83 μM) with pan-inhibitory activity against type I PRMTs. CM112 induces proteasome-dependent degradation of PRMT1, inhibits the methyltransferase activities of PRMT1, PRMT3, PRMT4 and PRMT6, downregulates the stability of orphan receptor TR3, thereby interfering with the non-enzymatic scaffolding function of PRMT1. CM112 suppresses clonogenicity and proliferation of tumor cells. CM112 is applicable to research related to breast cancer and non-small cell lung cancer.

PROTAC CARM1 degrader-1 is a highly selective CARM1 PROTAC degrader, with a DC₅₀ of 8.1 nM in MCF‑7 cells. PROTAC CARM1 degrader-1 recruits the VHL E3 ubiquitin ligase complex to act on CARM1, inducing a proteasome-dependent degradation process. PROTAC CARM1 degrader-1 downregulates the methylation level of CARM1 substrates in breast cancer cells, inhibits breast cancer cell migration, and exhibits no significant inhibitory effect on cell proliferation. PROTAC CARM1 degrader-1 is applicable for related research on breast cancer.

C199 is a PROTAC degrader targeting PRMT4 (DC₅₀ = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity.