EPZ015666
Cat. No.：YN310183
CAS No. ：1616391-65-1
| 产品名称: | EPZ015666 |
| CAS No.: | 1616391-65-1 |
| Chemical Name: | N-[(2S)-3-(3,4-dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide |
| Synonyms: | GSK3235025 |
| 分子量: | 383.44 |
| 分子式: | C₂₀H₂₅N₅O₃ |
| SMILES: | O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4COC4)=NC=N3 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | EPZ015666 (GSK3235025) 是有口服活性的PRMT5抑制剂，IC50为 22 nM。 |
| IC50和靶点: | |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Bissinger, E.M., Heinke, R., Sippl, W., et al.Targeting epigenetic modifiers: Inhibitors of histone methyltransferasesMed. Chem. Commun.1(2),(2010)
Copeland, R.A., Solomon, M.E., and Richon, V.M.Protein methyltransferases as a target class for drug discoveryNat. Rev. Drug Discov.8,724-732(2009)
Li, Y., Chitnis, N., Nakagawa, H., et al.PRMT5 is required for lymphomagenesis triggered by multiple oncogenic driversCancer Discov.5,288-303(2015)
Chung, J., Karkhanis, V., Tae, S., et al.Protein arginine methyltransferase 5 (PRMT5) inhibition induces lymphoma cell death through reactivation of the retinoblastoma tumor suppressor pathway and polycomb repressor complex 2 (PRC2) silencingJ. Biol. Chem.288(49),35534-35547(2013)
Chan-Penebre, E., Kuplast, K.G., Majer, C.R., et al.A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL modelsNat. Chem. Biol.11(6),432-437(2015)
