1. Signaling Pathways
  2. Epigenetics
  3. Histone Methyltransferase
  4. PRMT3 Isoform

PRMT3

PRMT3 (protein arginine methyltransferase 3) is a type I protein arginine methyltransferase that catalyzes asymmetric dimethylation of arginine residues and functions as a ribosomal protein methyltransferase involved in ribosome biogenesis and cellular protein synthesis regulation[1][2]. Mechanistically, PRMT3 is distinguished within the PRMT family by the presence of a zinc-finger domain that mediates substrate interaction, enabling regulation of diverse proteins involved in transcriptional control, post-transcriptional regulation, translation, and metabolic signaling pathways[3]. Through these activities, PRMT3 contributes to the control of gene expression and cellular metabolism, linking arginine methylation to fundamental biological processes[3]. In disease contexts, accumulating evidence indicates that PRMT3 participates in oncogenic programs by promoting metabolic reprogramming and gene expression changes associated with tumorigenesis[3]. Experimental studies further demonstrate that PRMT3 can influence cellular metabolism through regulation of glycolytic pathways and other metabolic processes relevant to cancer progression[3]. Compared with related PRMT isoforms, PRMT3 exhibits distinct substrate recognition, subcellular functions, and regulatory mechanisms, highlighting its nonredundant biological role[1][3]. For experimental applications, the allosteric inhibitor SGC707 provides a highly selective chemical probe for PRMT3, exhibiting nanomolar potency and substantial selectivity over other methyltransferases, thereby enabling mechanistic studies of PRMT3-dependent signaling and metabolic regulation[4]. Pharmacological inhibition of PRMT3 has also shown effects on hepatic triglyceride metabolism in preclinical models, supporting its utility for pathway interrogation and therapeutic target validation studies[5].

PRMT3 Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-19615
    MS023
    Inhibitor 99.93%
    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.
  • HY-128717A
    GSK3368715 dihydrochloride
    Inhibitor 99.96%
    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.
  • HY-19715
    SGC707
    Inhibitor 99.99%
    SGC707, a chemical probe, is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC50=31 nM, Kd=53 nM).
  • HY-128717
    GSK3368715
    Inhibitor 99.41%
    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-19615B
    MS023 dihydrochloride
    Inhibitor 99.68%
    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.
  • HY-141877
    MS4322
    Degrader 99.14%
    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 )).
  • HY-141877B
    MS4322 (isomer)
    99.87%
    MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 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 )).
  • 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-159728
    PROTAC PRMT3 degrader 1
    Degrader
    PROTAC PRMT3 degrader 1 is a selective PRMT3 PROTAC degrader with a DC50 of 2.566 μM. PROTAC PRMT3 degrader 1 forms a ternary complex with MDM2 E3 ubiquitin ligase to induce proteasomal and neddylation-dependent degradation of PRMT3. PROTAC PRMT3 degrader 1 activates intrinsic apoptosis, endoplasmic reticulum stress signaling pathways. PROTAC PRMT3 degrader 1 downregulates E2F, MYC, oxidative phosphorylation pathways. PROTAC PRMT3 degrader 1 reduces cellular asymmetric dimethylarginine (ADMA) levels. PROTAC PRMT3 degrader 1 inhibits acute leukemia cell growth. PROTAC PRMT3 degrader 1 acts with glycolysis inhibitor 2-DG to reduce ATP production, induce intrinsic apoptosis, drive synergistic antiproliferative effects. PROTAC PRMT3 degrader 1 can be used for the research of acute leukemia.
  • HY-175821
    PRMT1-IN-3
    Inhibitor
    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.
  • HY-159732
    PRMT3-IN-4
    Inhibitor
    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.
  • HY-171132
    PRMT3-IN-5
    Inhibitor
    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.
  • HY-161334
    CARM1-IN-4
    Inhibitor
    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.
  • HY-110158
    UNC2327
    Inhibitor 99.70%
    UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).