EPZ015666 GSK3235025

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Chemical Information

Product name：EPZ015666 GSK3235025	Purity：98% min
CAS NO：1616391-65-1	Solubility：DMSO : 100 mg/mL (260.80 mM)
Molecular Formula：C₂₀H₂₅N₅O₃	Package：Package according to customer requirements
Molecular Weight：383.444	Storage：Store at 2-8°C

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Remarks

EPZ015666, also known as GSK3235025, is a potent and selective and orally active PRMT5 inhibitor with a half-maximal inhibitory concentration (IC50) of 22 nM and broad selectivity against a panel of other histone methyltransferases. Treatment of MCL cell lines with EPZ015666 led to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range. Oral dosing with EPZ015666 demonstrated dose-dependent antitumor activity in multiple MCL xenograft models. EPZ015666 represents a validated chemical probe for further study of PRMT5 biology and arginine methylation in cancer and other diseases.

Histone Methyltransferase Inhibitors Related Products:

EPZ005687; GSK343; Tazemetostat; UNC1999; MM-102; SGC0946; SGC2085; OICR-9429; HLCL-61 HCL; GSK591; SGC707; GSK503; PFI-2 HCl; UNC0642; UNC0638; GSK-126; EPZ004777; GSK3326595; LLY-507; BRD4770 ; Pinometostat

References

[1]. Chan-Penebre E, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat Chem Biol. 2015 Jun;11(6):432-7.

[2]. Kryukov GV, et al. MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells. Science. 2016 Mar 11;351(6278):1214-8.