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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.
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