WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407273
Description: GSK591, also known as EPZ015866 and GSK3203591, is a chemical probe for PRMT5. In an in vitro biochemical assay, GSK591 potently inhibits the PRMT5/MEP50 complex from methylating (histone) H4 with IC50 = 11 nM. In Z-138 cells, GSK591 inhibits the symmetric arginine methylation of SmD3 with EC50 = 56 nM. Further, GSK591 is selective for PRMT5 (up to 50 micromolar) relative to a panel of methyltransferases. (http://www.thesgc.org/chemical-probes/GSK59).
MedKoo Cat#: 407273
Chemical Formula: C22H28N4O2
Exact Mass: 380.2212
Molecular Weight: 380.492
Elemental Analysis: C, 69.45; H, 7.42; N, 14.73; O, 8.41
Synonym: GSK591; GSK-591; GSK 591; EPZ015866; EPZ-015866; EPZ 015866; GSK 3203591; GSK-3203591; GSK3203591.
IUPAC/Chemical Name: (S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide
InChi Key: TWKYXZSXXXKKJU-FQEVSTJZSA-N
InChi Code: InChI=1S/C22H28N4O2/c27-20(15-26-11-9-16-4-1-2-5-18(16)14-26)13-24-22(28)17-8-10-23-21(12-17)25-19-6-3-7-19/h1-2,4-5,8,10,12,19-20,27H,3,6-7,9,11,13-15H2,(H,23,25)(H,24,28)/t20-/m0/s1
SMILES Code: O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4CCC4)=NC=C3
Protein arginine methyltransferases (PRMTs) play a crucial role in a variety of biological processes . Overexpression of PRMTs has been implicated in various human diseases including cancer. To date, nine PRMTs have been identified and they are grouped into three categories: types I, II and III. Type II PRMTs, 5 and 9, catalyze symmetric dimethylation of arginine residues, however, PRMT5 is the predominant enzyme for this process. PRMT5 interacts with a number of binding partners that influence its substrate specificity. In particular, MEP50, a member of the WD40 family of proteins, is required for PRMT5 methyltransferase activity. (http://www.thesgc.org/chemical-probes/GSK59)