Compound name
GSK591
Protein family
HMT
Target name
PRMT5
Affinity biochemical (nM)
4
Affinity on-target cellular (nM)
3
CG-Set
Epigenetic set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000198b
SMILES
O=C(NC[C@H](O)CN1CCc2ccccc2C1)c1ccnc(NC2CCC2)c1
InChIKey
TWKYXZSXXXKKJU-FQEVSTJZSA-N
NCBI gene ID
10419
UniProt ID
O14744
Synonyms
HRMT1L5, HSL7, IBP72, JBP1, SKB1, SKB1Hs
Mode of action
Inhibitor
Negative control
SGC2096
Affinity biochemical definition
IC50
Affinity biochemical assay type
HTRF assay (monomethylation of H4R3 on a histone H4 peptide by PRMT5:MEP50)
Affinity Biochemical Source Knowledge
https://doi.org/10.1021/acsmedchemlett.5b00380
Affinity biochemical relation
=
Affinity on-target cellular definition
IC50
Affinity on-target cellular assay type
In-Cell Western (ICW) format assay (inhibition of symmetric arginine methylation of SmD3 in Z-138 cells)
Affinity on-target cellular relation
=
Selectivity platform
Methyltransferase panel, literature
Selectivity platform number of targets
32
Selectivity remarks
Screened at 1 and 10 µM, closest target NSD3 (75% at 10 µM), GSK591 is highly selective
Selectivity Source Knowledge
https://www.thesgc.org/chemical-probes/GSK591
Selectivity Number of Off-targets
0