EPZ015666 , 10mMinDMSO , 1616391-65-1
Synonym(s):
(S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide;GSK3235025;YQ36286
| Pack Size | Price | Stock | Quantity |
| 1ml | RMB559.20 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 124-131°C |
| Boiling point: | 686.4±55.0 °C(Predicted) |
| Density | 1.331±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | Soluble in DMSO (up to 20 mg/ml) |
| pka | 12.40±0.46(Predicted) |
| form | powder |
| color | white to beige |
| Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Description and Uses
EPZ015666 (1616391-65-1) is a selective and potent (IC50?= 22nM) inhibitor of arginine methyltransferase 5 (PRMT5).1,2?PRMT5 inhibition with EPZ015666 potently suppressed?in vivo?glioblastoma tumors3?and significantly inhibited the growth of multiple myeloma cell lines4.
Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression. PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas. Moreover, suppression of PRMT5 expression induces lymphoma cell death. EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM). It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.[Cayman Chemical]
