2. シグナル伝達
  3. Epigenetics
  4. Histone Methyltransferase
  5. PRMT4 Isoform

PRMT4

PRMT4, also known as coactivator-associated arginine methyltransferase 1 (CARM1), is a type I protein arginine methyltransferase that functions as a transcriptional coactivator and epigenetic regulator through arginine methylation of histone and non-histone substrates[1][2]. CARM1 was originally characterized by its ability to catalyze asymmetric dimethylation of histone H3 at arginine residues associated with chromatin remodeling and transcriptional activation, thereby linking arginine methylation to gene expression control[1][3]. Beyond chromatin regulation, CARM1 methylates diverse non-histone proteins involved in RNA processing, transcriptional regulation, metabolism, autophagy, and organelle dynamics, positioning the enzyme as a multifunctional regulator of cellular homeostasis[1][2][4]. Mechanistically, CARM1 participates in pathways governing transcription, mRNA splicing, RNA metabolism, cell-cycle regulation, metabolic adaptation, and NF-κB signaling, extending its biological influence beyond canonical nuclear functions[1][2][4]. In disease contexts, aberrant CARM1 expression or activity has been associated with tumorigenesis, metastasis, and therapeutic resistance across multiple cancer types, supporting its relevance as a therapeutic target and experimental biomarker[2][5][6]. Compared with other PRMT family members, CARM1 displays distinctive substrate specificity, preferentially targeting arginine residues located within proline-, glycine-, and methionine-rich sequences rather than the glycine-arginine-rich motifs favored by many related PRMTs[1][7]. Alternative splicing further distinguishes CARM1 biology, as full-length and exon 15-deficient isoforms exhibit different subcellular localization patterns and cancer-associated functions[1][4]. For experimental applications, selective CARM1 inhibitors, including EZM2302 and TP-064, have enabled pharmacological interrogation of CARM1-dependent pathways, although emerging evidence indicates that catalytic inhibition may not fully suppress nonenzymatic scaffolding functions of the protein[1][6].

PRMT4 関連製品 (15):

製品番号 製品名 製品効果 純度
  • 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-114965
    TP-064 Inhibitor 99.29%
    TP-064, a chemical probe, 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-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-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-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-183653
    AK442 Inhibitor
    AK442 is a selective PRMT4 (CARM1) inhibitor with an IC50 of 2.6 nM against human targets. AK442 is applicable to breast cancer-related research.
  • HY-12759
    CARM1-IN-1 Inhibitor
    CARM1-IN-1 (compound 7g) is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity.
  • HY-100360
    MS049 Inhibitor 98.0%
    MS049, a chemical probe, 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-12759A
    CARM1-IN-1 hydrochloride Inhibitor
    CARM1-IN-1 (compound 7g) hydrochloride is a highly potent and selective inhibitor of CARM1 (IC50=8.6 μM, CARM1/PABP1), with low inhibitory activity against PRMT1 and SET7 (IC50 >667 μM). CARM1-IN-1 hydrochloride inhibits the methylation activity of CARM1 and the methylation levels of different substrates, such as PABP1, CA150, SmB, and H3. CARM1-IN-1 hydrochloride also inhibits the promoter activity of prostate-specific antigen (PSA) without significant cytotoxicity.
  • 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-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.
  • 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-174445
    C199 Degrader
    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 (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker).