Home Methylation PRMT inhibitor GSK3368715 3HCl For research use only.

GSK3368715 3HCl

Synonyms: EPZ019997 3HCl

GSK3368715 3HCl 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.

GSK3368715 3HCl Chemical Structure

GSK3368715 3HCl Chemical Structure

CAS: 2227587-26-8

Selleck's GSK3368715 3HCl has been cited by 5 publications

Purity & Quality Control

Batch: S885801 DMSO] 81 mg/mL] false] Water] 81 mg/mL] false] Ethanol] 81 mg/mL] false Purity: 98.88%
98.88

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Biological Activity

Description GSK3368715 3HCl 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
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]
Cell Research 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.
In Vivo
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]
Animal Research 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

Chemical Information & Solubility

Molecular Weight 475.92 Formula

C20H41Cl3N4O2
CAS No. 2227587-26-8 SDF --
Smiles Cl.Cl.Cl.CCOCC1(CCC(CC1)C2=N[NH]C=C2CN(C)CCNC)COCC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 81 mg/mL ( (170.19 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 81 mg/mL

Ethanol : 81 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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.

Handling Instructions

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