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Chemical Structure : EPZ015666
CAS No.: 1616391-65-1
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $98 | In stock | |
| 10 mg | $148 | In stock | |
| 25 mg | $248 | In stock | |
| 50 mg | $398 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 383.4442 | |
| Formula | C20H25N5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: 10 mM (3.8 mg/mL) |
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| Chemical Name/SMILES |
4-Pyrimidinecarboxamide, N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)- |
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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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