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MS117

Cat. No. M21482
MS117  Structure
Size Price Availability
5mg USD 350  USD350 1-2 Weeks
10mg USD 580  USD580 1-2 Weeks
25mg USD 1100  USD1100 1-2 Weeks
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Quality Control & Documentation
Biological Activity

MS117 is a first-in-class, cell-active, irreversible covalent inhibitor of protein arginine methyltransferase (PRMT6) with an IC50 value of 18 nM.

Chemical Information
Molecular Weight 298.38
Formula C17H22N4O
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Corey B Hughes, et al. Cell Tissue Res. Impact of an SGLT2-loss of function mutation on renal architecture, histology, and glucose homeostasis

[2] Yudao Shen, et al. J Med Chem. Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor

[3] Steven R Presnell, et al. Int Immunol. Functional redundancy of transcription factor-binding sites in the killer cell Ig-like receptor (KIR) gene promoter

[4] J L Winters, et al. J Neurol Sci. Congenital glioblastoma multiforme: a report of three cases and a review of the literature

[5] T Suzuki, et al. Mol Microbiol. Complementation of an Enterococcus hirae (Streptococcus faecalis) mutant in the alpha subunit of the H(+)-ATPase by cloned genes from the same and different species

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  Catalog
Abmole Inhibitor Catalog




Keywords: MS117 supplier, Histone Methyltransferase, inhibitors, activators


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