GSK3368715 (EPZ019997) 3HCl

For research use only.

Catalog No.S8858 Synonyms: GSK3368715 (EPZ019997)

GSK3368715 (EPZ019997) 3HCl Chemical Structure

CAS No. 2227587-26-8

GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.

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Biological Activity

Description GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
Targets
PRMT1 [1]
()
PRMT3 [1]
()
PRMT4 [1]
()
PRMT6 [1]
()
PRMT8 [1]
()
In vitro

GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.[1]

In vivo

GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: 249 cancer cell lines (Toledo cells, BxPC3 cells, MiaPaca-2 cells, ACHN cells, MDA-MB-468 cells, RKO cells, Panc03.27 cells, etc.)
  • Concentrations: 0.75 nM, 2 μM
  • Incubation Time: 30 min, 3 h - 168 h
  • Method: In Cell Western. RKO cells are seeded in a clear bottom 384 well plates andtreated with a 20-point two-fold dilution series of GSK3368715 (29,325.5 to 0.03 nM) or 0.15% DMSO. Plates are incubated for 3 days at 37℃ in 5% CO2. Cells are fixed with ice-cold methanol for 30 minutes at room temperature, washed with phosphate buffered saline (PBS), then incubated with Odyssey blocking buffer (Licor) for 1 hour at room temperature.
    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female NMRI nu/nu mice (NMRI-Foxn1nu) implanted with tumor fragment
  • Dosages: 75 mg/kg, 150 mg/kg, 300 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 81 mg/mL (170.19 mM)
Water 81 mg/mL (170.19 mM)
Ethanol '81 mg/mL

* 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.

Chemical Information

Molecular Weight 475.92
Formula

C20H41Cl3N4O2

CAS No. 2227587-26-8
Storage powder
in solvent
Synonyms GSK3368715 (EPZ019997)

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID