PRMT3 Inhibitor

MS023, a chemical probe, is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC₅₀s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC₅₀=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

SGC707, a chemical probe, is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC₅₀=31 nM, K_d=53 nM).

GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC₅₀=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC₅₀s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.

MS3-123 is an orally active PRMT1 inhibitor (IC₅₀ = 11.4 nM) that selectively targets the unique Cys119 residue within the SAM-binding pocket. MS3-123 covalently binds to PRMT1 through a time-dependent irreversible mechanism and exhibits high selectivity over other PRMT family members and other methyltransferases. MS3-123 inhibits breast cancer cell proliferation, migration and invasion, and induces cell cycle arrest and apoptosis. MS3-123 is useful for breast cancer research.

GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC₅₀=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

PRMT4-IN-1 is a selective inhibitor of PRMT4 (IC₅₀=3.2 nM). PRMT4-IN-1 inhibits MCF7 relative viability.

PRMT1-IN-3 is a potent protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 4.11 μM. PRMT1-IN-3 inhibits PRMT6 and PRMT8 with IC₅₀s of 23.3 and 30.1 μM. PRMT1-IN-3 suppresses asymmetric dimethylarginine (ADMA) levels and histone H4R3me2a modification in triple-negative breast cancer (TNBC) cells. PRMT1-IN-3 induces cell cycle arrest, apoptosis, and inhibits migration and colony formation in MDA-MB-231 cells. PRMT1-IN-3 acts as chemotherapeutic sensitizers for Paclitaxel (HY-B0015). PRMT1-IN-3 can be used for the study of TNBC.

PRMT3-IN-4 (intermediate 15) is a protein arginine methyltransferase 3 (PRMT3) inhibitor. PRMT3-IN-4 is an active control for HY-19715. PRMT3-IN-4 can be used to synthesize PROTACs targeting PRMT3. PRMT3-IN-4 can be used in leukemia-related research.

PRMT3-IN-5 (Compound 14) is an allosteric PRMT3 inhibitor (IC₅₀: 291 nM). PRMT3-IN-5 can be used for investigating PRMT3's biological functions and disease associations.

CARM1-IN-4 (compound 11f) is a potent CARM1 inhibitor with IC₅₀s of 9 nM and 56 nM for CARM1 and PRMT1, respectively. CARM1-IN-4 displays significant anti-proliferative effects on colorectal cancer cell lines. CARM1-IN-4 effectively inhibits the methyltransferase activity of CARM1 and prevents methylation of downstream proteins. CARM1-IN-4 induces apoptosis and shows antitumor activity.

UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).