MS023 trihydrochloride

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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.

For research use only. We do not sell to patients.

MS023 trihydrochloride Chemical Structure

CAS No. : 2108631-19-0

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Other In-stock Forms of MS023 trihydrochloride:

MS023

Other Forms of MS023 trihydrochloride:

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11 Publications Citing Use of MCE MS023 trihydrochloride

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•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

Biological Activity
Purity & Documentation
References
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Description

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 nM).Treatment concentration-dependently reduced the H3R2me2a mark (IC₅₀=56 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.

Molecular Weight

396.78

Formula

C₁₇H₂₈Cl₃N₃O

CAS No.

2108631-19-0

SMILES

CC(OC1=CC=C(C=C1)C2=CNC=C2CN(CCN)C)C.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]