Art. -Nr.: HY-19615

MS023

24 Cited Publications

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Based on 24 publication(s) in Google Scholar

MS023, a chemical probe, 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.

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Reinheit: 99.93%
CAS. Nr.: 1831110-54-3
Formel: C₁₇H₂₅N₃O
Molecular Weight:287.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS023 Chemical Structure

CAS. Nr.: 1831110-54-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PRMT1

PRMT3

PRMT6

PRMT8

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	13.4 μM Compound: Chemical probe: MS023	Antiproliferative against human A549 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM) Antiproliferative against human A549 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)	[PMID: 33691794]
A549	IC₅₀	5.1 μM Compound: Chemical probe: MS023	Antiproliferative against human A549 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM) Antiproliferative against human A549 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 4.4 uM)	[PMID: 33691794]
HCC4006	IC₅₀	0.47 μM Compound: Chemical probe: MS023	Antiproliferative against human HCC4006 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM) Antiproliferative against human HCC4006 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)	[PMID: 33691794]
HCC4006	IC₅₀	0.56 μM Compound: Chemical probe: MS023	Antiproliferative against human HCC4006 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM) Antiproliferative against human HCC4006 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 0.24 uM)	[PMID: 33691794]
SK-LU-1	IC₅₀	36.7 μM Compound: Chemical probe: MS023	Antiproliferative against human SK-LU-1 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM) Antiproliferative against human SK-LU-1 cells expressing MTAP clone 1 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)	[PMID: 33691794]
SK-LU-1	IC₅₀	41 μM Compound: Chemical probe: MS023	Antiproliferative against human SK-LU-1 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM) Antiproliferative against human SK-LU-1 cells expressing MTAP clone 2 assessed as reduction of cell death treated for 7 days with replenishment of medium for every 48 hrs by MTT assay (Rvb = 16.3 uM)	[PMID: 33691794]

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

MCF7 and HEK293 cells
Concentration:

1.4, 4, 12, 37, 111, 333, and 1000 nM
Incubation Time:

48 hours for MCF7 cells; 20 hours for HEK293 cells
Result:

Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC₅₀=9±0.2 nM).
Treatment concentration-dependently reduced the H3R2me2a mark (IC₅₀=56±7 nM).

In Vivo

Administration of MS023 (160 mg/kg, i.p) in combination with PKC412 (100 mg/kg, i.g.) blocks MLL-r acute lymphoblastic leukemia (ALL) propagation by inhibiting maintenance of functional MLL-r ALL-initiating cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells^[2]
Dosage:

160 mg/kg
Administration:

Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
Result:

Combinatorial treatment extended survival of leukemic mice relative to single treatments.

Chemical Information

CAS. Nr. 1831110-54-3
Appearance Solid
Molecular Weight 287.40
Formel C₁₇H₂₅N₃O
Color White to light yellow
SMILES

CN(CCN)CC1=CNC=C1C2=CC=C(OC(C)C)C=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (24)

All Cell Imaging/StainingCell Proliferation/Viability AssayWBIPRT-PCR

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Journal Impact Factor

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

PRMT1-methylated MSX1 phase separates to control palate development. [Abstract]

2025 Jan 22;16(1):949. PMID: 39843447

MS023 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 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.
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
Nucleic Acids Res

RECQ4 arginine methylation suppresses single-stranded DNA gap accumulation at replication forks. [Abstract]

2026 Jun 22;54(12):gkag655. PMID: 42363758
Acta Pharm Sin B

Prmt1 upregulated by Hdc deficiency aggravates acute myocardial infarction via NETosis. [Abstract]

2022 Apr;12(4):1840-1855. PMID: 35847488
Cell Rep Med

Sequence-dependent splicing dysregulation drives therapy resistance in pediatric AML. [Abstract]

2026 Jan 20;7(1):102542. PMID: 41564858

MS023 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 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.
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 Commun Signal

Specific sDMA modifications on the RGG/RG motif of METTL14 regulate its function in AML. [Abstract]

2025 Mar 8;23(1):126. PMID: 40057764

MS023 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.
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
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
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
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
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
EMBO Rep

Tudor-based proteomic strategy pan-specifically enriches and identifies protein arginine methylation. [Abstract]

2025 Oct 20. PMID: 41116072
EMBO Rep

Arginine methylation-dependent METTL14-SMN interaction regulates RNA m6A homeostasis. [Abstract]

2025 Oct 6. PMID: 41053315
Oncogenesis

Methylation of HBP1 by PRMT1 promotes tumor progression by regulating actin cytoskeleton remodeling. [Abstract]

2022 Aug 8;11(1):45. PMID: 35941115
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
Bone

PRMT1-mediated arginine methylation promotes postnatal calvaria bone formation through BMP-Smad signaling. [Abstract]

2023 Nov:176:116887. PMID: 37634683
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
PLoS One

Asymmetric and symmetric protein arginine methylation in methionine-addicted human cancer cells. [Abstract]

2023 Dec 22;18(12):e0296291. PMID: 38134182
bioRxiv

2026 May 29.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (347.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4795 mL

17.3974 mL

34.7947 mL

5 mM

0.6959 mL

3.4795 mL

6.9589 mL

10 mM

0.3479 mL

1.7397 mL

3.4795 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Saline

Solubility: 53.33 mg/mL (185.56 mM); Clear solution; Need ultrasonic and adjust pH to 8 with 1M HCl

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4795 mL	17.3974 mL	34.7947 mL	86.9868 mL
	5 mM	0.6959 mL	3.4795 mL	6.9589 mL	17.3974 mL
	10 mM	0.3479 mL	1.7397 mL	3.4795 mL	8.6987 mL
	15 mM	0.2320 mL	1.1598 mL	2.3196 mL	5.7991 mL
	20 mM	0.1740 mL	0.8699 mL	1.7397 mL	4.3493 mL
	25 mM	0.1392 mL	0.6959 mL	1.3918 mL	3.4795 mL
	30 mM	0.1160 mL	0.5799 mL	1.1598 mL	2.8996 mL
	40 mM	0.0870 mL	0.4349 mL	0.8699 mL	2.1747 mL
	50 mM	0.0696 mL	0.3479 mL	0.6959 mL	1.7397 mL
	60 mM	0.0580 mL	0.2900 mL	0.5799 mL	1.4498 mL
	80 mM	0.0435 mL	0.2175 mL	0.4349 mL	1.0873 mL
	100 mM	0.0348 mL	0.1740 mL	0.3479 mL	0.8699 mL

Keywords

MS023

24 Cited Publications

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MS023

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library Mini

Epigenetics Compound Library

Publications Citing Use of MedChemExpress (MCE) MS023

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS023

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Epigenetics Compound Library Mini

Epigenetics Compound Library

Publications Citing Use of MedChemExpress (MCE) MS023

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MS023 Related Classifications

HY-19615 Related Classifications