MS023 trihydrochloride
Based on 24 publication(s) in Google Scholar
MS023 trihydrochloride 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 2108631-19-0
- Formel: C17H28Cl3N3O
- Molecular Weight:396.78
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MS023 trihydrochloride
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2025 Jan 22;16(1):949. [Abstract]
- Nat Commun. 2025 Jan 2;16(1):87. [Abstract]
- Acta Pharm Sin B. 2022 Apr;12(4):1840-1855. [Abstract]
- Nucleic Acids Res. 2026 Jun 22;54(12):gkag655. [Abstract]
- Sci Adv. 2026 Jan 23;12(4):eaea3960. [Abstract]
- Cell Rep Med. 2026 Jan 20;7(1):102542. [Abstract]
- Cell Commun Signal. 2025 Mar 8;23(1):126. [Abstract]
- Int J Biol Macromol. 2024 Aug 1:134411. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- Cell Rep. 2024 Jul 24;43(8):114537. [Abstract]
- Cell Rep. 2021 Sep 21;36(12):109731. [Abstract]
- J Med Chem. 2025 Feb 27;68(4):4373-4381. [Abstract]
- Oncogenesis. 2022 Aug 8;11(1):45. [Abstract]
- EMBO Rep. 2025 Oct 20. [Abstract]
- EMBO Rep. 2025 Oct 6. [Abstract]
- Cell Mol Life Sci. 2025 Apr 7;82(1):142. [Abstract]
- Eur J Med Chem. 2025 Dec 15:300:118123. [Abstract]
- Cancer. 2024 Apr 15;130(S8):1415-1423. [Abstract]
- Neurochem Int. 2024 Jun:176:105728. [Abstract]
- J Proteome Res. 2024 Mar 1;23(3):1014-1027. [Abstract]
- Bone. 2023 Nov:176:116887. [Abstract]
- PLoS One. 2023 Dec 22;18(12):e0296291. [Abstract]
- bioRxiv. 2026 May 29.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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RT-PCR
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Cell Imaging/Staining
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IP
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WB
Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells[1].
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 and HEK293 cells
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Concentration:1.4, 4, 12, 37, 111, 333, and 1000 nM
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Incubation Time:48 hours for MCF7 cells; 20 hours for HEK293 cells
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Result:Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC50=9 nM).Treatment concentration-dependently reduced the H3R2me2a mark (IC50=56 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells[2]
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Dosage:160 mg/kg
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Administration:Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
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Result:Combinatorial treatment extended survival of leukemic mice relative to single treatments.
Chemical Information
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CAS. Nr. 2108631-19-0
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Molecular Weight 396.78
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Formel C17H28Cl3N3O
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SMILES
CC(OC1=CC=C(C=C1)C2=CNC=C2CN(CCN)C)C.Cl.Cl.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (24)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Nat Commun
2025 Jan 22;16(1):949. PMID: 39843447
MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):949. [Abstract]
Representative images of FRAP of MSX1-mEGFP- expressing HEK293T treated with DMSO or MS023.
MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):949. [Abstract]
Representative western blot images of Co-IP assays assessing the aDMA of MSX1 in treated with MS023 or PRMT1 siRNA.
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Nat Commun
Positive feedback between arginine methylation of YAP and methionine transporter SLC43A2 drives anticancer drug resistance. [Abstract]2025 Jan 2;16(1):87. PMID: 39747898 -
Acta Pharm Sin B
2022 Apr;12(4):1840-1855. PMID: 35847488 -
Nucleic Acids Res
RECQ4 arginine methylation suppresses single-stranded DNA gap accumulation at replication forks. [Abstract]2026 Jun 22;54(12):gkag655. PMID: 42363758 -
Sci Adv
TDRD3, a Tudor domain-containing protein, regulates Klf2-dependent Treg differentiation and function to modulate immune tolerance. [Abstract]2026 Jan 23;12(4):eaea3960. PMID: 41576154 -
Cell Rep Med
2026 Jan 20;7(1):102542. PMID: 41564858
MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102542. [Abstract]
The drug response curve and IC50 value for PRMT inhibitor MS023 and GSK591 combinations after U2AF2 knockdown in THP1 leukemia cells. Cell viability was assessed using a CCK8 assay.
MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 Jan 20;7(1):102542. [Abstract]
RT-PCR results detecting aberrantly spliced transcripts in THP1 leukemia cells, which were treated with PRMT inhibitor MS023 or GSK591 with or without U2AF2 knockdown.
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Cell Commun Signal
2025 Mar 8;23(1):126. PMID: 40057764
MS023 trihydrochloride purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2025 Mar 8;23(1):126. [Abstract]
Immunoprecipitation and western blot analysis of arginine dimethylation in METTL14 overexpressed in HEK293T cells. Cells were treated with 1 μM EPZ015666, 1 μM MS023, or DMSO for 72 h and METTL14 is immunoprecipitated by anti-METTL14 antibody.
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Int J Biol Macromol
PRMT1 and TDRD3 promote stress granule assembly by rebuilding the protein-RNA interaction network. [Abstract]2024 Aug 1:134411. PMID: 39097054 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
Cell Rep
Arginine methylation-enabled FUS phase separation with SMN contributes to neuronal granule formation. [Abstract]2024 Jul 24;43(8):114537. PMID: 39052476 -
Cell Rep
The protein arginine methyltransferase PRMT1 promotes TBK1 activation through asymmetric arginine methylation. [Abstract]2021 Sep 21;36(12):109731. PMID: 34551290 -
J Med Chem
Opto-Epigenetic Regulation of Histone Arginine Asymmetric Dimethylation via Type I Protein Arginine Methyltransferase Inhibition. [Abstract]2025 Feb 27;68(4):4373-4381. PMID: 39961800 -
Oncogenesis
Methylation of HBP1 by PRMT1 promotes tumor progression by regulating actin cytoskeleton remodeling. [Abstract]2022 Aug 8;11(1):45. PMID: 35941115 -
EMBO Rep
Tudor-based proteomic strategy pan-specifically enriches and identifies protein arginine methylation. [Abstract]2025 Oct 20. PMID: 41116072 -
EMBO Rep
2025 Oct 6. PMID: 41053315 -
Cell Mol Life Sci
Dietary advanced glycation end-products exacerbate sarcopenia onset by activating apoptosis through PRMT1-mediated CRTC3 arginine methylation. [Abstract]2025 Apr 7;82(1):142. PMID: 40192801 -
Eur J Med Chem
Discovery of novel indazole derivatives as type Ⅰ PRMTs inhibitors for the treatment of triple-negative breast cancer. [Abstract]2025 Dec 15:300:118123. PMID: 40929806 -
Cancer
Type-I protein arginine methyltransferase inhibition primes anti-programmed cell death protein 1 immunotherapy in triple-negative breast cancer. [Abstract]2024 Apr 15;130(S8):1415-1423. PMID: 38079306 -
Neurochem Int
The antidepressant effects of protein arginine methyltransferase 2 involve neuroinflammation. [Abstract]2024 Jun:176:105728. PMID: 38561150 -
J Proteome Res
ETD-Based Proteomic Profiling Improves Arginine Methylation Identification and Reveals Novel PRMT5 Substrates. [Abstract]2024 Mar 1;23(3):1014-1027. PMID: 38272855 -
Bone
PRMT1-mediated arginine methylation promotes postnatal calvaria bone formation through BMP-Smad signaling. [Abstract]2023 Nov:176:116887. PMID: 37634683 -
PLoS One
Asymmetric and symmetric protein arginine methylation in methionine-addicted human cancer cells. [Abstract]2023 Dec 22;18(12):e0296291. PMID: 38134182 -
Reinheit & Dokumentation
Verweise
[1]. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81. [Content Brief]
[2]. Yinghui Zhu, et al. Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia. Blood. 2019 Oct 10;134(15):1257-1268. [Content Brief]
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