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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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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CMP-5
0 ImagesCMP-5 is a potent, specific, and selective PRMT5 inhibitor, while displays no activity against PRMT1, PRMT4, and PRMT7 enzymes. CMP-5 selectively blocks S2Me-H4R3 by inhibiting PRMT5 methyltransferase activity on histone preparations. CMP-5 prevents Epstein-Barr virus (EBV)-driven B-lymphocyte transformation but leaving normal B cells unaffected.
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AZD3470
0 ImagesAZD3470 is an orally active MTA-cooperative PRMT5 inhibitor, selective for MTAP-deficient tumors. AZD3470 induces cell cycle G2/M phase alterations, DNA damage, apoptosis, and symmetric dimethylarginine reduction. AZD3470 alters alternative splicing, increases skipped exon events in DNA repair and cell cycle pathways, and inhibits cancer cell proliferation and tumor growth. AZD3470 can be used for the research of non-small cell lung cancer and MTAP-deleted solid tumors.
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PRMT5-IN-1 hydrochloride
0 ImagesCat. No.: HY-126256APurity: 99.51%PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
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WX2-43
0 ImagesWX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer.
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PRMT5-IN-1
0 ImagesCat. No.: HY-126256CAS No.: 2366149-83-7
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MRTX9768 hydrochloride
0 ImagesMRTX9768 hydrochloride is a potent, selective, orally active, first-in-class PRMT5-MTA complex inhibitor.
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PRT543
0 ImagesCat. No.: HY-141876CAS No.: 2278356-90-2PRT543 is an orally active selective PRMT5 inhibitor. PRT543 reduces intracellular symmetric dimethylarginine (sDMA) levels, downregulates the expression of genes related to DNA damage repair and DNA replication pathways, and induces abnormal alternative splicing. PRT543 inhibits the MYB, NOTCH1 and PI3K/AKT signaling pathways, promotes nuclear translocation of FOXO1, upregulates the pro-apoptotic protein BAX, and enhances cellular sensitivity to BCL-2 inhibition. PRT543 disrupts the normal RNA splicing process and exerts a synthetic lethal effect on myeloid tumor cells carrying splicing factor mutations. PRT543 can be used in research related to various cancers including breast cancer, ovarian cancer and acute myeloid leukemia.
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PRMT5-MTA-IN-1
0 ImagesCat. No.: HY-163799CAS No.: 3048425-88-0PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice.
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PRMT5-IN-39-d3
0 ImagesCat. No.: HY-163587CAS No.: 3034033-85-4
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RAPRMT5
0 ImagesCat. No.: HY-181521CAS No.: 2721998-42-9
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PRMT5-IN-57
0 ImagesCat. No.: HY-184434CAS No.: 3064280-41-4PRMT5-IN-57 is an orally active andselective MTA-cooperative PRMT5 inhibitor, with an IC50 of 8.39 nM against PRMT5/MTA complex. PRMT5-IN-57 exhibits potent and selective antiproliferative activity against MTAP-null cancer cells. PRMT5-IN-57 demonstrates significant in vivo antitumor efficacy in an HCT116 MTAP-/- CDX model. PRMT5-IN-57 can be used for the research of MTAP-deleted cancers.
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PARP1/PRMT5-IN-1
0 ImagesCat. No.: HY-189242CAS No.: 3133817-84-9PARP1/PRMT5-IN-1 is an inhibitor of PARP1 and PRMT5, with an IC50 of 0.60 nM against PARP1 and an IC50 of 4.67 nM against PRMT5. PARP1/PRMT5-IN-1 downregulates the homologous recombination (HR)-associated factors BRCA1, BRCA2, and RAD51, thereby suppressing homologous recombination function. PARP1/PRMT5-IN-1 induces the accumulation of DNA double-strand breaks. PARP1/PRMT5-IN-1 triggers apoptosis. PARP1/PRMT5-IN-1 is applicable for breast cancer research.
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PRMT5-IN-28
0 ImagesCat. No.: HY-153421CAS No.: 2242753-66-6PRMT5-IN-28 (compound 36) is an inhibitor of protein arginine methyltransferase 5 (PRMT5) enzyme. Protein arginine methylation is a common post-translational modification involved in gene transcription, mRNA splicing, DNA repair, protein cellular localization, cell fate determination and signal transduction, etc. Abnormal PRMT5 can promote cancer cell proliferation, resist apoptosis, enhance invasion and metastasis, and affect immune escape.
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PRMT5-IN-52
0 ImagesCat. No.: HY-176534CAS No.: 2783961-64-6PRMT5-IN-52 (Compound 17) is a non-nucleoside Protein Arginine Methyltransferase 5 (PRMT5) inhibitor with inhibitory rates of 20.2% at 10 μM. PRMT5-IN-52 has potent antitumor activity, promising for research of cancers, including lung, prostate cancer, and colorectal carcinoma.
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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-47
0 ImagesCat. No.: HY-168842CAS No.: 3065081-87-7PRMT5-IN-47 (compound 20) is a potent, selectively and orally active, MTA cooperative PRMT5 inhibitor with an IC50 value of 15 nM. PRMT5-IN-47 shows antiproliferative activity. PRMT5-IN-47 shows anticancer activity.
