EPZ015866 (GSK591) | B1216

EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5/MEP50 complex thus stopping the methylation of histone H4 with IC₅₀ of 11 nM. It also maintains superior selectivity against other panels of methyl transferases inhibiting the symmetric arginine methylation of SmD3 with EC₅₀ of 56 nM.

EPZ015866 (GSK591) is a potent selective inhibitor of the arginine methyltransferase PRMT5/MEP50 complex thus stopping the methylation of histone H4 with IC₅₀ of 11 nM. It also maintains superior selectivity against other panels of methyl transferases inhibiting the symmetric arginine methylation of SmD3 with EC₅₀ of 56 nM.

B1216 | EPZ015866 (GSK591) DataSheet

Alternate Name/Synonyms: (S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide

Appearance: Crystalline solid

Formulation: N/A

CAS Number: 1616391-87-7

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₂H₂₈N₄O₂

Molecular Weight: 380.5

Cell-Permeable?: Yes

Purity: ≥98% by HPLC

Solubilities: DMSO(>40 mg/ml)

Handling: Protect from air and light

Country of Origin: USA

Tag Line: A potent selective inhibitor of the arginine methyltransferase PRMT5/MEP50 complex

MDL Number: N/A

PubChem CID: 117072552

SMILES: C1CC(C1)NC2=NC=CC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)O

InChi: 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

InChi Key: TWKYXZSXXXKKJU-FQEVSTJZSA-N