EPZ015866 GSK591

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Chemical Information

Product name：EPZ015866 GSK591	Purity：99% min
CAS NO：1616391-87-7	Solubility：DMSO : ≥ 135 mg/mL (354.81 mM)
Molecular Formula：C₂₂H₂₈N₄O₂	Package：Package according to customer requirements
Molecular Weight：380.483	Storage：Store at 2-8°C

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Remarks

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.

Histone Methyltransferase Inhibitors Related Products:

EPZ005687; GSK343; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; HLCL-61 HCL; SGC707; GSK503; EPZ015666; PFI-2 HCl; UNC0642; UNC0638; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770 ; Pinometostat

References

[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]. [2] Elayne Chan-Penebre et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nature Chemical Biology 11, 2015, 432-437