2. Signaling Pathways
  3. Epigenetics
  4. Histone Methyltransferase
  5. PRMT4 Isoform
  6. PRMT4 Inhibitor

PRMT4 Inhibitor

PRMT4 Inhibitors (8):

Cat. No. Product Name Effect Purity
  • HY-114965
    TP-064
    		Inhibitor 99.61%
    TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities.
  • HY-100565
    SGC2085
    		Inhibitor 99.46%
    SGC2085 is a potent and selective inhibitor of coactivator associated arginine methyltransferase 1 (CARM1) with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
  • HY-100360
    MS049
    		Inhibitor ≥98.0%
    MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells.
  • HY-128717
    GSK3368715
    		Inhibitor
    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.
  • HY-12759A
    CARM1-IN-1 hydrochloride
    		Inhibitor
    CARM1-IN-1 hydrochloride is a potent and specific CARM1 (Coactivator-associated arginine methyltransferase 1) inhibitor with IC50 of 8.6 uM; shows very low activity against PRMT1 and SET7.
  • HY-128717B
    GSK3368715 trihydrochloride
    		Inhibitor
    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.
  • HY-146810
    PRMT4-IN-1
    		Inhibitor
    PRMT4-IN-1 is a selective inhibitor of PRMT4 (IC50=3.2 nM). PRMT4-IN-1 inhibits MCF7 relative viability.
  • HY-149005
    PRMT5-IN-19
    		Inhibitor
    PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research.