SKU: C-1132-5mg
C20H25N5O3  Solid Powder
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  • Catalog#: C-1132
  • Quantity: 5mg
  • Targets: PRMT5
  • Synonym: EPZ015666; EPZ-015666; EPZ 015666; GSK3235025; GSK-3235025; GSK 3235025
  • Chemical Name/IUPAC:(S)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
    Technical Data
  • Product Name: EPZ-015666
  • Chemical Formula: C20H25N5O3
  • Molecular Weight: 383.45
  • CAS#: 1616391-65-1
  • Appearance: Solid powder
  • Purity: > 99% by HPLC
  • Solubility: Soluble in DMSO
  • Storage: Room temperature for months, or -20ºC for 3 years
    EPZ-015666 (GSK3235025) is a potent and selective and orally active PRMT5 inhibitor with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ-015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ-015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ-015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.