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Merck
CN

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

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About This Item

Empirical Formula (Hill Notation):
C20H25N5O3
CAS Number:
1616391-65-1
Molecular Weight:
383.44
MDL number:
MFCD28411588
UNSPSC Code:
12352200
PubChem Substance ID:
329825864
NACRES:
NA.77

Key Documents

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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

Related Categories

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.
EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor.

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000224203
0000224203
0000180198
0000177860
0000180198

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Rosemary Millen et al.
Med (New York, N.Y.), 4(5), 290-310 (2023-05-14)
Organoids are in vitro three-dimensional structures that can be grown from patient tissue. Head and neck cancer (HNC) is a collective term used for multiple tumor types including squamous cell carcinomas and salivary gland adenocarcinomas. Organoids were established from HNC patient
Zhengxin Wang et al.
Molecular and cellular biology, 42(4), e0052321-e0052321 (2022-03-22)
Protein arginine methyltransferase (PRMT) enzymes catalyze posttranslational modifications of target proteins and are often upregulated in human cancers. In this study, we purified two chemical compounds from seeds of Foeniculum vulgare based on their ability to inhibit the enzymatic activity
Maneka Chitiprolu et al.
Nature communications, 9(1), 2794-2794 (2018-07-20)
Mutations in proteins like FUS which cause Amyotrophic Lateral Sclerosis (ALS) result in the aberrant formation of stress granules while ALS-linked mutations in other proteins impede elimination of stress granules. Repeat expansions in C9ORF72, the major cause of ALS, reduce
Pan-methylarginine antibody generation using PEG linked GAR motifs as antigens.
Wang, et al.
Methods, 200, 80-86 (2023)
Kazuki Fukumoto et al.
Communications biology, 5(1), 313-313 (2022-04-07)
The global dietary supplement market is valued at over USD 100 billion. One popular dietary supplement, S-adenosylmethionine, is marketed to improve joints, liver health and emotional well-being in the US since 1999, and has been a prescription drug in Europe
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