SML1421

EPZ015666

≥98% (HPLC)

• Synonym(s): (S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide, GSK3235025, YQ36286
• Empirical Formula (Hill Notation): C₂₀H₂₅N₅O₃
• CAS Number: 1616391-65-1
• Molecular Weight: 383.44
• MDL number: MFCD28411588
• PubChem Substance ID: 329825864
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: O[C@H](CN1CCC(C=CC=C2)=C2C1)CNC(C3=CC(NC4COC4)=NC=N3)=O
• InChI: 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-/m0/s1
• InChI key: ZKXZLIFRWWKZRY-KRWDZBQOSA-N

Description

Packaging

5, 25 mg in glass bottle

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.

Safety Information

• Storage Class Code: 13 - Non Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable