PRMT5
Protein arginine methyltransferase 5 (PRMT5) is a type II arginine methyltransferase that catalyzes symmetric dimethylation of arginine residues on histone and non-histone substrates, thereby regulating chromatin organization, transcriptional control, and cellular development[1][2]. PRMT5 functions as a major epigenetic regulator through symmetric methylation marks such as H3R8me2s and H4R3me2s, which influence gene expression programs and growth-regulatory pathways[1][3]. Mechanistically, PRMT5 plays a central role in RNA processing and alternative splicing, and has been identified as a master regulator of mammalian splicing networks, linking arginine methylation to transcriptome regulation[4][5]. Therefore, PRMT5 integrates transcriptional and post-transcriptional regulation to control cell proliferation, differentiation, survival, and genome maintenance[1][5]. In disease settings, PRMT5 is frequently overexpressed or hyperactivated in multiple cancers, where it supports tumor cell growth, metastasis, and therapeutic resistance through regulation of oncogenic signaling, transcription, and RNA metabolism[2][5][6]. Compared with related isoforms, PRMT5 belongs to the type II PRMT family and primarily generates symmetric dimethylarginine, whereas PRMT1 is the major type I enzyme responsible for asymmetric dimethylarginine formation, highlighting distinct but partially overlapping biological functions[3][7]. For experimental applications, PRMT5 has emerged as a therapeutic target, and pharmacological inhibition disrupts methyltransferase-dependent signaling and splicing pathways; recent MTA-cooperative inhibitors further exploit vulnerabilities in MTAP-deleted tumors[5][6]. These characteristics make PRMT5 an important model for studying epigenetic regulation, RNA splicing, and targeted cancer therapy[1][4][6].
References:
- [1]. Stopa N, et al. The PRMT5 arginine methyltransferase: many roles in development, cancer and beyond. Cell Mol Life Sci. 2015 Jun;72(11):2041-59. [Content Brief]
- [2]. Lee J, et al. Targeting PRMT5 in cancer: Mechanistic insights and clinical progress. Biomed Pharmacother. 2025 Dec;193:118754. [Content Brief]
- [3]. Shailesh H, et al. Protein arginine methyltransferase 5 (PRMT5) dysregulation in cancer. Oncotarget. 2018 Nov 30;9(94):36705-36718. [Content Brief]
- [4]. Bezzi M, et al. Regulation of constitutive and alternative splicing by PRMT5 reveals a role for Mdm4 pre-mRNA in sensing defects in the spliceosomal machinery. Genes Dev. 2013 Sep 1;27(17):1903-16. [Content Brief]
- [5]. Kim H, et al. PRMT5 function and targeting in cancer. Cell Stress. 2020 Jul;4(8):199-215. [Content Brief]
- [6]. Hwang JW, et al. Protein arginine methyltransferases: promising targets for cancer therapy. Exp Mol Med. 2021 May;53(5):788-808. [Content Brief]
- [7]. Gao G, et al. PRMT1 loss sensitizes cells to PRMT5 inhibition. Nucleic Acids Res. 2019 Jun 4;47(10):5038-5048. [Content Brief]
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PRMT5 Related Products (63)
Related Products (63)
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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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PRMT5 ligand 3
0 ImagesCat. No.: HY-181522CAS No.: 1616397-61-5PRMT5 ligand 3 (Compound S19) is a PRMT5 ligand that can be used for the synthesis of PROTACs, such as RAPRMT5 (HY-181521).
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PRMT5-IN-20 hydrochloride
0 ImagesCat. No.: HY-111213ACAS No.: 1047976-55-5
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PRMT5-MTA-IN-4
0 ImagesCat. No.: HY-176701CAS No.: 3025838-18-7PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma.
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PRMT5-IN-54
0 ImagesCat. No.: HY-180356CAS No.: 2242788-68-5PRMT5-IN-54 (example 92a) is a protein arginine methyltransferase 5 (PRMT5) inhibitor. PRMT5-IN-54 can be used for the study of autoimmune diseases.
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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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PRMT5-IN-43
0 ImagesCat. No.: HY-163592CAS No.: 3034746-11-4
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PRMT5-MTA-IN-5
0 ImagesCat. No.: HY-176702CAS No.: 3078322-88-7PRMT5-MTA-IN-5 (Compound 7) is an orally active, irreversible PRMT5-MTA complex (PRMT5•MTA) inhibitor (IC50=1.15 nM). PRMT5-MTA-IN-5 blocks arginine methylation and inhibits ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-5 potently inhibits proliferation in MTAP-deficient tumor cells. PRMT5-MTA-IN-5 is promising for research of MTAP-deficient solid tumors, such as liver, breast, and pancreatic cancers.
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PRMT5-IN-44
0 ImagesCat. No.: HY-163593CAS No.: 3034746-35-2
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PRMT5-IN-9
0 ImagesCat. No.: HY-132937CAS No.: 2691869-52-8PRMT5-IN-9 is a novel PRMT5 inhibitor for researching cancer, with an IC50 of 0.01 μM.
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CARM1-IN-4
0 ImagesCat. No.: HY-161334CAS No.: 2878481-07-1CARM1-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.
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PRMT5-IN-49
0 ImagesCat. No.: HY-169708CAS No.: 428853-17-2PRMT5-IN-49 (Compound 4b16) is an inhibitor of PRMT5.
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PRMT5-IN-33
0 ImagesCat. No.: HY-162230CAS No.: 3054228-62-2
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PRMT5-IN-21
0 ImagesCat. No.: HY-150081CAS No.: 2922673-38-7PRMT5-IN-21 (compound 1) is a potent cyclonucleoside PRMT5 inhibitor.
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PRMT5-IN-36-d3
0 ImagesCat. No.: HY-163591CAS No.: 3034034-10-8PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research.
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PRMT5-IN-53
0 ImagesCat. No.: HY-178028CAS No.: 3113303-04-8PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP).
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YZ-17
0 ImagesCat. No.: HY-189213YZ-17 is a PROTAC degrader targeting PRMT5, with DC50 = 2.2 μM (HCC1806 cells). YZ-17 recruits CRBN E3 ligase and induces PRMT5 degradation through the ubiquitin-proteasome system, inhibiting PRMT5-mediated symmetric dimethylarginine modification. YZ-17 co-degrades the PRMT5 adaptor protein MEP50 via a CRBN-dependent mechanism. YZ-17 induces G1 phase cell cycle arrest and inhibits colony formation in cancer cells. YZ-17 exhibits antiproliferative activity in various cancer cells. YZ-17 shows antitumor efficacy in a triple-negative breast cancer xenograft mouse model. YZ-17 can be used for research on triple-negative breast cancer.
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PRMT5-IN-58
0 ImagesCat. No.: HY-189289CAS No.: 3107304-24-2PRMT5-IN-58 is an MTA-cooperative PRMT5 inhibitor and PRMT5-MTA complex binder (IC50 = 11.7 nM) that inhibits methyltransferase activity and SDMA (HY-101410) production by stabilizing the MTA-bound conformation, and induces apoptosis via sub-G1 phase accumulation, exhibiting selective antiproliferative activity against MTAP-deleted cancer cells over MTAP wild-type cells. PRMT5-IN-58 can be used for research on MTAP-deleted cancers.
