2. Epigenetics
  3. Histone Methyltransferase
  4. MS023 trihydrochloride

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.

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MS023 trihydrochloride Chemical Structure

MS023 trihydrochloride Chemical Structure

CAS No. : 2108631-19-0

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MS023 trihydrochloride Related Antibodies

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Description

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[1].

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.

MS023 trihydrochloride Related Antibodies

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.
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
References
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MS023 trihydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS023 trihydrochloride2108631-19-0Histone MethyltransferaseInhibitorinhibitorinhibit

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