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SML1421 Sigma-Aldrich

EPZ015666

≥98% (HPLC)

Synonym: (S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide, GSK3235025, YQ36286

  • CAS Number 1616391-65-1

  • Empirical Formula (Hill Notation) C20H25N5O3

  • Molecular Weight 383.44

  •  MDL number MFCD28411588

  •  PubChem Substance ID 329825864

  •  NACRES NA.77

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, DNA-RNA Transcription Regulators,
InChI Key   ZKXZLIFRWWKZRY-KRWDZBQOSA-N
Quality Level   100
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 20 mg/mL, clear
storage temp.   2-8°C

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 & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis (COA)

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Protocols & Articles
Peer-Reviewed Papers
15

References

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