Product Name :
GSK591 (EPZ015866), PRMT5 Inhibitor
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.
CAS:
1616391-87-7
Molecular Weight:
380.48
Formula:
C22H28N4O2
Chemical Name:
(S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide
Smiles :
O[C@@H](CNC(=O)C1=CC(NC2CCC2)=NC=C1)CN1CCC2=CC=CC=C2C1
InChiKey:
TWKYXZSXXXKKJU-FQEVSTJZSA-N
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
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Oteseconazole} web|{Oteseconazole} Metabolic Enzyme/Protease|{Oteseconazole} Purity & Documentation|{Oteseconazole} Data Sheet|{Oteseconazole} custom synthesis|{Oteseconazole} Epigenetic Reader Domain}
Additional information:
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.|Product information|CAS Number: 1616391-87-7|Molecular Weight: 380.48|Formula: C22H28N4O2|Chemical Name: (S)-2-(cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide|Smiles: O[C@@H](CNC(=O)C1=CC(NC2CCC2)=NC=C1)CN1CCC2=CC=CC=C2C1|InChiKey: TWKYXZSXXXKKJU-FQEVSTJZSA-N|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|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO: 76 mg/mL(199.74 mM). Water: Insoluble.|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Sulindac} MedChemExpress|{Sulindac} NF-κB|{Sulindac} Biological Activity|{Sulindac} In Vivo|{Sulindac} custom synthesis|{Sulindac} Cancer} |Shelf Life: ≥12 months if stored properly.PMID:23291014 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|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.|References:|SGC. GSK591 A chemical probe for PRMT5.Elayne Chan-Penebre, et al. Nat Chem Biol. 2015, 11(6):432-437.Duncan KW, et al. ACS Med Chem Lett. 2016, 7(2):162-166.Products are for research use only. Not for human use.|Documents||
