Cookie Policy: This site uses cookies to improve your experience. You can find out more about our use of cookies in our Privacy Policy. By continuing to browse this site you agree to our use of cookies.
SynKinase
EPZ015666
CHF 0.00
In stock
SYN-3044-M0011 mgCHF 114.00
SYN-3044-M0055 mgCHF 213.00
SYN-3044-M01010 mgCHF 355.00
SYN-3044-M05050 mgCHF 1'064.00
SYN-3044-M100100 mgINQ
| Product Details | |
|---|---|
| Synonyms | GSK3235025; YQ36286; (S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide |
| Product Type | Chemical |
| Properties | |
| Formula | C20H25N5O3 |
| MW | 383.4 |
| CAS | 1616391-65-1 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data | Target: PRMT5 | Kinase Group: N/A | Substrate: N/A |
| InChi Key | ZKXZLIFRWWKZRY-KRWDZBQOSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS | Inquire |
| Product Specification Sheet | |
| Datasheet |
 Download PDF |
Description
Protein arginine methyltransferase-5 (PRMT5) is reported to have a role in diverse cellular processes, including tumorigenesis and its overexpression is observed in cell lines and primary patient samples derived from lymphomas, particularly mantle cell lymphoma (MCL). EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity in biochemical assays with an IC50 of 22nM 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. 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.
Product References
- A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models: E. Chan-Penebre, et al.; Nat. Chem. Biol. 11, 432 (2015)
- Species differences in metabolism of EPZ015666, an oxetane-containing protein arginine methyltransferase-5 (PRMT5) inhibitor: N. Rioux, et al.; Xenobiotica 46, 268 (2016)