PRMT1
Protein arginine methyltransferase 1 (PRMT1) is the primary type I PRMT responsible for asymmetric dimethylation of arginine residues on histone and non-histone proteins[1][2]. Mechanistically, PRMT1 regulates gene transcription, RNA processing, DNA replication, and signal transduction pathways critical for cell proliferation and survival[3][2]. PRMT1 activity influences type I interferon signaling and modulates anti-tumor immunity, particularly in lung adenocarcinoma, affecting proliferation, migration, and invasion[4]. In disease models, PRMT1 dysregulation contributes to persistence of cancer cells under EGFR- and KRAS-targeted therapies, with knockdown enhancing drug efficacy and prolonging tumor regression in xenografts[5]. Compared with related isoforms, PRMT1 exhibits distinct substrate specificity and nuclear localization, unlike PRMT3 which is primarily cytoplasmic, or PRMT8 which has brain-specific expression[6][7]. Functionally, PRMT1 shows sensitivity to ionic strength, temperature, and pH, allowing regulation under cellular stress conditions[2]. Experimental applications have demonstrated that inhibition of PRMT1, alone or combined with PRMT5 blockade, sensitizes cancer cells to DNA damage and PARP inhibitors, highlighting its therapeutic potential[8][9]. Collectively, PRMT1 is a key epigenetic regulator, distinct from other PRMT isoforms, and serves as a critical target in cancer biology and therapeutic design[10][5].
References:
- [1]. Wang YC, et al. Identification, chromosomal arrangements and expression analyses of the evolutionarily conserved prmt1 gene in chicken in comparison with its vertebrate paralogue prmt8. PLoS One. 2017 Sep 21;12(9):e0185042. [Content Brief]
- [2]. Lowe TL, et al. Human protein arginine methyltransferases (PRMTs) can be optimally active under nonphysiological conditions. J Biol Chem. 2022 Sep;298(9):102290. [Content Brief]
- [3]. Yoshimatsu M, et al. Dysregulation of PRMT1 and PRMT6, Type I arginine methyltransferases, is involved in various types of human cancers. Int J Cancer. 2011 Feb 1;128(3):562-73. [Content Brief]
- [4]. Wang J, et al. Pan-cancer analysis identifies protein arginine methyltransferases PRMT1 and PRMT5 and their related signatures as markers associated with prognosis, immune profile, and therapeutic response in lung adenocarcinoma. Heliyon. 2023 Nov 27;9(12):e22088. [Content Brief]
- [5]. Sun X, et al. Targeting PRMT1 Reduces Cancer Persistence and Tumor Relapse in EGFR- and KRAS-Mutant Lung Cancer. Cancer Res Commun. 2025 Jan 1;5(1):119-127. [Content Brief]
- [6]. Tang J, et al. PRMT 3, a type I protein arginine N-methyltransferase that differs from PRMT1 in its oligomerization, subcellular localization, substrate specificity, and regulation. J Biol Chem. 1998 Jul 3;273(27):16935-45. [Content Brief]
- [7]. Lin YL, et al. The critical role of protein arginine methyltransferase prmt8 in zebrafish embryonic and neural development is non-redundant with its paralogue prmt1. PLoS One. 2013;8(3):e55221. [Content Brief]
- [8]. Zhang Y, et al. Repression of PRMT activities sensitize human homologous recombination-proficient ovarian and breast cancer cells to PARP inhibitor treatment. Elife. 2026 Feb 3;13:RP99225. [Content Brief]
- [9]. Gao G, et al. PRMT1 loss sensitizes cells to PRMT5 inhibition. Nucleic Acids Res. 2019 Jun 4;47(10):5038-5048. [Content Brief]
- [10]. Li M, et al. The arginine methyltransferase PRMT5 and PRMT1 distinctly regulate the degradation of anti-apoptotic protein CFLARL in human lung cancer cells. J Exp Clin Cancer Res. 2019 Feb 8;38(1):64. [Content Brief]
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PRMT1 Related Products (24)
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Antibodies (1)
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GSK3368715 dihydrochloride
0 ImagesSynonyms: EPZ019997 dihydrochlorideGSK3368715 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.
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TC-E 5003
0 ImagesTC-E 5003 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 1.5 µM against hPRMT1. TC-E 5003 modulates the lipopolysaccharide (LPS) (HY-D1056)-induced AP-1 and NF-κB signaling pathways with anti-inflammatory properties. TC-E 5003 also upregulates the expression of Ucp1 and Fgf21, activates protein kinase A signaling and lipolysis in primary subcutaneous adipocytes from both mouse and humans. TC-E 5003 is promising for research of obesity and associated metabolic disorders, oxidative stress, inflammation and cancers.
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GSK3368715
0 ImagesSynonyms: EPZ019997GSK3368715 (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.
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SKLB06489
0 ImagesCat. No.: HY-186045SKLB06489 is a selective and orally active inhibitor of type I PRMT enzymes, with IC50 values of 64.55 nM (PRMT1), 4.21 nM (PRMT6), and 51.27 nM (PRMT8). SKLB06489 inhibits cell proliferation, colony formation, DNA replication, and DNA damage repair in cancer cells. SKLB06489 induces G0/G1-phase cell cycle arrest and apoptosis in cancer cells. SKLB06489 enhances intracellular cholesterol efflux via ABCA1 and ABCG1 upregulation, disrupts cholesterol metabolic homeostasis, and suppresses tumor growth in subcutaneous xenograft models. SKLB06489 can be used for the research of triple-negative breast cancer (TNBC).
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MS3-123
0 ImagesCat. No.: HY-184653MS3-123 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.
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Furamidine dihydrochloride
0 ImagesSynonyms: DB75 dihydrochloride; NSC 305831 dihydrochlorideFuramidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.
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MS4322
0 ImagesSynonyms: YS43-22MS4322 (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 )).
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DCLX069
0 ImagesDCLX069 is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 value of 17.9 µM. DCLX069 shows less active against PRMT4 and PRMT6. DCLX069 has anticancer effects.
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MS4322 (isomer)
0 ImagesSynonyms: YS43-22 (isomer)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.
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AMI-408
0 ImagesCat. No.: HY-164456CAS No.: 78866-14-5AMI-408 is a PRMT1 inhibitor. AMI-408 can reduce H4R3me2as level in MLL-GAS7 leukemia cells.
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CM112
0 ImagesCat. No.: HY-172769CM112 is a selective protein arginine methyltransferase 1 (PRMT1) degrader by tethering hydrophobic tag, adamantane, to MS023 with a 5-PEG linker. CM112 induces the degradation of PRMT1 in various solid cancer cell lines. CM112 can also target the nonenzymatic function of PRMT1 by downregulating the stability of the orphan receptor TR3. CM112 is promising for research of cancers.
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GSK3368715 trihydrochloride
0 ImagesCat. No.: HY-128717BCAS No.: 2227587-26-8Synonyms: EPZ019997 trihydrochlorideGSK3368715 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.
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PRMT4-IN-1
0 ImagesCat. No.: HY-146810CAS No.: 3035425-70-5PRMT4-IN-1 is a selective inhibitor of PRMT4 (IC50=3.2 nM). PRMT4-IN-1 inhibits MCF7 relative viability.
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PRMT5-IN-19
0 ImagesCat. No.: HY-149005CAS No.: 2783961-86-2PRMT5-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.
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PRMT1-IN-3
0 ImagesCat. No.: HY-175821CAS No.: 892570-48-8PRMT1-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.
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