1. Epigenetics
  2. Histone Methyltransferase
  3. MS023

MS023 

Cat. No.: HY-19615 Purity: 99.73%
COA Handling Instructions

MS023 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 Chemical Structure

MS023 Chemical Structure

CAS No. : 1831110-54-3

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
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Solid
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of MS023:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MS023 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].

IC50 & Target

PRMT1

 

PRMT3

 

PRMT6

 

PRMT8

 

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.
Molecular Weight

287.40

Formula

C17H25N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (104.38 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.73%

References
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MS023 Related Classifications

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.

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  • Dilution Calculator

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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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Product Name:
MS023
Cat. No.:
HY-19615
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