GSK591 (EPZ015866), PRMT5 Inhibitor


Catalog No. size PriceQuantity
M60321-2S 2 mg solid $109
M60321-10S 10mg solid $431

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.

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.

Shelf Life: ≥12 months if stored properly.

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:

  1. SGC. GSK591 A chemical probe for PRMT5.
  2. Elayne Chan-Penebre, et al. Nat Chem Biol. 2015, 11(6):432-437.
  3. Duncan KW, et al. ACS Med Chem Lett. 2016, 7(2):162-166.

Products are for research use only. Not for human use.


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