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EPZ015666

Chemical Structure : EPZ015666

CAS No.: 1616391-65-1

EPZ015666 (EPZ-015666;GSK3235025)

Catalog No.: PC-43165Not For Human Use, Lab Use Only.

EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM, displays broad selectivity against a panel of other histone methyltransferases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

EPZ015666 (GSK3235025) is a potent, selective, orally available inhibitor of PRMT5 with Ki/IC50 of 5/22 nM, displays broad selectivity against a panel of other histone methyltransferases.
EPZ015666 (GSK3235025) inhibits SmD3 methylation and causes cell death in MCL cell lines (IC50=61-904 nM).
EPZ015666 (GSK3235025) demonstrates potent concentration-dependent antiproliferative effects against Z-138 and Maver-1 cells with IC50 of 96 and 450 nM, respectively.
EPZ015666 (GSK3235025) exhibits antitumor activity in multiple MCL xenograft models.

Physicochemical Properties

M.Wt 383.4442
Formula C20H25N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 10 mM (3.8 mg/mL)

Chemical Name/SMILES

4-Pyrimidinecarboxamide, N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-

References

1. Chan-Penebre E, et al. Nat Chem Biol. 2015 Jun;11(6):432-7.

2. Kryukov GV, et al. Science. 2016 Mar 11;351(6278):1214-8.

3. Chan-Penebre E, et al. ACS Med Chem Lett. 2015 Dec 2;7(2):162-6.

4. Gullà A, et al. Leukemia. 2018 Apr;32(4):996-1002.

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