For research use only. Not for therapeutic Use.
GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM[1].
GSK591 (5 μM; MCF7, T47D, and MCF10A cells) treatment suppresses breast cancer stem cells (BCSCs) proliferation and self-renewal. GSK591 reduces BCSCs numbers in vitro[2].
| Catalog Number | I013766 |
| CAS Number | 1616391-87-7 |
| Synonyms | 2-(cyclobutylamino)-N-[(2S)-3-(3,4-dihydro-1H-isoquinolin-2-yl)-2-hydroxypropyl]pyridine-4-carboxamide |
| Molecular Formula | C22H28N4O2 |
| Purity | ≥95% |
| 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 |
| InChIKey | TWKYXZSXXXKKJU-FQEVSTJZSA-N |
| SMILES | C1CC(C1)NC2=NC=CC(=C2)C(=O)NCC(CN3CCC4=CC=CC=C4C3)O |
| Reference | [1]. [1] Kenneth W. Duncan et al. Structure and Property Guided Design in the Identification of PRMT5 Tool Compound EPZ015666. ACS Med. Chem. Lett., 2016, 7 (2), pp 162-166. [2]. Chiang K, et al. PRMT5 Is a Critical Regulator of Breast Cancer Stem Cell Function via Histone Methylation and FOXP1 Expression. Cell Rep. 2017 Dec 19;21(12):3498-3513. |
