EPZ015666

EPZ015666

Biochem/physiol Actions

EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor with an IC50 value of of 22 nM in biochemical assays and no inhibition up to the maximum tested concentration of 50 µM against a panel of 20 other protein methyltransferases. Inhibition was uncompetitive with respect to SAM. EPZ015666 showed dose-dependent antitumor activity in multiple in vitro and in vivo mantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death.

Other Notes

EPZ015666 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the EPZ015666 probe summary on the Chemical Probes Portal website.

Packaging

5, 25 mg in glass bottle

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Code Description Colour Quality Level InChI key InChI Manufacturer Solubility Form Assay Price Quantity
3574889 EPZ015666 white to beige 100 ZKXZLIFRWWKZRY-KRWDZBQOSA-N 1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-
£927.64 (exc VAT) per 25MG
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3574890 EPZ015666 white to beige 100 ZKXZLIFRWWKZRY-KRWDZBQOSA-N 1S/C20H25N5O3/c26-17(10-25-6-5-14-3-1-2-4-15(14)9-25)8-21-20(27)18-7-19(23-13-22-18)24-16-11-28-12-16/h1-4,7,13,16-17,26H,5-6,8-12H2,(H,21,27)(H,22,23,24)/t17-
£299.46 (exc VAT) per 5MG
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