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EPZ015666 | Potent and selective PRMT5 inhibitor

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.

References/Citations

1) Chan-Penebre et al. (2015), A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models; Nat. Chem. Biol. 11 432
2) Duncan et al. (2015), Structure and Property Guided Design in the Identification of PRMT5 Toll Compound EPZ015666; ACS Med. Chem. Lett. 7 162
3) Braun et al. (2017), Coordinated Splicing of Regulatory Detained Introns within Oncogenic Transcripts Creates an Exploitable Vulnerability in Malignant Glioma; Cancer Cell 32 411
4) Gulia et al. (2018), Protein arginine methyltransferase 5 has prognostic relevance and is a druggable target in multiple myeloma; Leukemia 32 996

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Catalog#  10-4031-0005

$110.00
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CAS:
1616391-65-1
Catalog Number:
10-4031
Activity:
Potent and selective PRMT5 inhibitor
Chemical Name:
(S)-N-(3-(3,4-Dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)-6-(oxetan-3-ylamino)pyrimidine-4-carboxamide
Molecular Weight:
383.44
Molecular Formula:
C20H25N5O3
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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