EPZ015666 (GSK3235025) - PRMT5 Inhibitor. CAS# 1616391-65-1 size:10 mg solid (2010) Neuropharmacology

(2010) Neuropharmacology

BG45 alone and in combination with bortezomib triggers significant tumor growth inhibition in vivo in a murine xenograft model of human MM

correlates with CK2α mRNA and protein levels but not the CK2α' catalytic subunit

DASA-58 (40 μM) treated cells are injected into male SCID-bg/bg mice bearing PC3 tumors by IV

CAS Number: 1355324-14-9

EPZ015666 (GSK3235025) - PRMT5 Inhibitor. CAS# 1616391-65-1 size:10 mg solid (2010) NeuropharmacologyEPZ015666, also known as GSK3235025, CAS No. 1616391 65 1, 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 EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose dependent