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LLY-283

Cat. No. M6312
LLY-283 Structure
Size Price Availability
10mg USD 260  USD260 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.

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 342.35
Formula C17H18N4O4
CAS Number 2040291-27-6
Purity >99%
Solubility 10 mM in DMSO
Storage at -20°C
References

[1] H. Ümit Kaniskan, et al. Chem Rev. Inhibitors of Protein Methyltransferases and Demethylases

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LLY-283 supplier, PRMTs, inhibitors

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