GSK3326595 (EPZ015938)

Background Information:

GSK3326595 (EPZ015938) is an orally active, potent, selective, SAM
uncompetitive, peptide competitive, slow binding inhibitor of protein
arginine methyltransferase 5 (PRMT5)/MEP50 with a biochemical IC50 of 6
nM (ref 1), and is >4,000-fold selective for PRMT5/MEP50 over any
other enzyme when tested in a panel containing 20 other histone
methyltransferases (ref 1). Display potent antitumor activities in vitro
and in vivo in animal models. It is currently in clinical evaluation
for the treatment of solid tumors and non-Hodgkin’s lymphoma.

Reference:

1. S.V. Gerhart, et al, Activation of the p53-MDM4 regulatory axis
defines the anti-tumour response to PRMT5 inhibition through its role in
regulating cellular splicing, Scientific Reports, volume 8, Article
number: 9711 (2018).

APIM050331: GSK3326595 (EPZ015938)

CAS No.: 1616392-22-3.
Molecular Formula: C24H32N6O3.
Molecular Weight: 452.6 (or refer to Certificate of Analysis, batch-specific).
Purity: 99.9% by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.