ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis.

EPZ032597 is a novel selective inhibitor of SMYD2 with an IC50 of 16 nM. EPZ032597 has anticancer activity and can be used to prevent and treat pancreatic cancer.

BBDDL2059 is a selective covalent inhibitor targeting EZH2, exhibiting an IC50 of 1.5 nM against the EZH2-Y641F mutant. It demonstrates potency in inhibiting lymphoma cell proliferation at nanomolar concentrations, proving its utility in anticancer research [1].

PROTAC CARM1 degrader-1 (compound 3b) serves as a highly potent degrader (DC50=8.1 nM) of the co-activator associated arginine methyltransferase (CARM1). This compound facilitates the degradation of CARM1 via the VHL-proteasome pathway. By degrading CARM1, PROTAC CARM1 degrader-1 effectively reduces the methylation of its substrates, including poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, subsequently inhibiting breast cancer cell migration [1].

Igermetostat, an EZH2 inhibitor, is utilized both in vivo and in vitro for cancer research [1].