EPZ015666 (GSK3235025)

Catalog No.S7748 Batch:S774802

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Technical Data

Formula

C20H25N5O3
Molecular Weight 383.44 CAS No. 1616391-65-1
Solubility (25°C)* In vitro DMSO 76 mg/mL (198.2 mM)
Ethanol 67 mg/mL (174.73 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description EPZ015666 (GSK3235025) is a potent, selective and orally bioavailable PRMT5 inhibitor with Ki of 5 nM, >20,000-fold selectivity over other PMTs.
Targets
PRMT5 [1]
(Cell-free assay)
5 nM(Ki)
In vitro

EPZ015666 shows potent cellular activity that blocks symmetric dimethylation of SmD3 and inhibit proliferation of MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1) with IC50 of 96-904 nM. [1]
In vivo

EPZ015666 (200 mg/kg, p.o.) displays robust anti-tumor activity in MCL xenograft animal models. [1]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MCL cell lines (Z-138, Granta-519, Maver-1, Mino, and Jeko-1)

  • Concentrations

    5 μM

  • Incubation Time

    12 days

  • Method

    --
Animal Study:

[1]
  • Animal Models

    MCL (Z-138, and Maver-1) xenograft models

  • Dosages

    200 mg/kg BID

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , J Cell Mol Med, 2016, 1-10.]

Selleck's EPZ015666 (GSK3235025) has been cited by 33 publications

Arginine methylation of caspase-8 controls life/death decisions in extrinsic apoptotic networks [ Oncogene, 2024, 10.1038/s41388-024-03049-6] PubMed: 38730267
Genetic screen identified PRMT5 as a neuroprotection target against cerebral ischemia [ Elife, 2024, 12RP89754] PubMed: 38372724
Methylation of KSHV vCyclin by PRMT5 contributes to cell cycle progression and cell proliferation [ PLoS Pathog, 2024, 20(9):e1012535] PubMed: 39255317
Development and validation of a generic methyltransferase enzymatic assay based on an SAH riboswitch [ SLAS Discov, 2024, 29(4):100161] PubMed: 38788976
Genome-wide mapping of cancer dependency genes and genetic modifiers of chemotherapy in high-risk hepatoblastoma [ Nat Commun, 2023, 14(1):4003] PubMed: 37414763
FACS-based genome-wide CRISPR screens define key regulators of DNA damage signaling pathways [ Mol Cell, 2023, 83(15):2810-2828.e6] PubMed: 37541219
PRMT blockade induces defective DNA replication stress response and synergizes with PARP inhibition [ Cell Rep Med, 2023, 4(12):101326] PubMed: 38118413
Inhibition of histone methyltransferase PRMT5 attenuates cisplatin-induced hearing loss through the PI3K/Akt-mediated mitochondrial apoptotic pathway [ J Pharm Anal, 2023, 13(6):590-602] PubMed: 37440906
(S)-2-(Cyclobutylamino)-N-(3-(3,4-dihydroisoquinolin-2(1H)-yl)-2-hydroxypropyl)isonicotinamide Attenuates RANKL-Induced Osteoclast Differentiation by Inhibiting NF-κB Nuclear Translocation [ Int J Mol Sci, 2023, 24(5)4327] PubMed: 36901758
SHARPIN Enhances Ferroptosis in Synovial Sarcoma Cells via NF-κB- and PRMT5-Mediated PGC1α Reduction [ Cancers (Basel), 2023, 15(13)3484] PubMed: 37444594

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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