EPZ-015666

SKU: C-1132

Made in USA, High-Purity Standard Quality

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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

Description
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.

EPZ-015666

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