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MS023

Cat. No. M9003
MS023 Structure
Synonym:

MS-023

Size Price Availability Quantity
5mg USD 125  USD125 In stock
10mg USD 225  USD225 In stock
25mg USD 415  USD415 In stock
50mg USD 760  USD760 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

MS023 potently inhibits PRMT1 (IC50 = 30 ± 9 nM), PRMT3 (IC50 = 119 ± 14 nM), PRMT4 (IC50 = 83 ± 10 nM), PRMT6 (IC50 = 4 ± 0.5 nM), and PRMT8 (IC50 = 5 ± 0.1 nM). MS023 displays high potency for type I PRMTs including PRMT1, -3, -4, -6, and -8 but is completely inactive against type II and type III PRMTs, protein lysine methyltransferases and DNA methyltransferases. MS023 potently decreases cellular levels of histone arginine asymmetric dimethylation. It also reduces global levels of arginine asymmetric dimethylation and concurrently increased levels of arginine monomethylation and symmetric dimethylation in cells.

Protocol
Cell Experiment
Cell lines MCF7, U2Os, HFF, HCT116, HEK293 , A549, MDA-MB-231 and T98G
Preparation method Different cell lines are seeded on 96-well plates at density 3000/well and treated with MS023 at 0, 0.1, 1, 10, 50 and 100 μM concentrations for 96 h. MCF7, U2Os, HFF, HCT116, HEK293 are grown in DMEM and A549, MDA-MB-231 and T98G in RPMI supplemented with 10% FBS, penicillin (100 U/mL) and streptomycin (100 mg/mL). The inhibitor is replaced after 48 h. The confluency is measured using IncuCyte™ ZOOM live cell imaging device and analysed with IncuCyte™ ZOOM (2015A) software based on phase contrast images.
Concentrations ~100 μM
Incubation time 96 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 287.40
Formula C17H25N3O
CAS Number 1831110-54-3
Purity >98%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
References

[1] Eram MS, et al. ACS Chem Biol. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

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  Catalog
Abmole Inhibitor Catalog




Keywords: MS023, MS-023 supplier, PRMTs, inhibitors

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