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GSK3368715 3HCl PRMT inhibitor

Name: GSK3368715 3HCl
Brand: Selleck Chemicals
SKU: S8858
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S8858

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

Chemical Structure

Molecular Weight: 475.92

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

98.88

Related Targets	EZH2 MAT2A DNA Methyltransferase LSD1 JMJD G9a/GLP MLL NSD FTO SETD
Other PRMT Inhibitors	LLY-283 GSK3326595 (Pemrametostat, EPZ015938) C7280948 TC-E 5003 BRD0639 Furamidine dihydrochloride LLY-284 TNG-462 AMG 193 MS023 hydrochloride

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (170.19 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 81 mg/mL

Ethanol : 81 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.050mg/ml (8.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 81 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.675mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	475.92	Formula	C₂₀H₄₁Cl₃N₄O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2227587-26-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EPZ019997 3HCl			Smiles	Cl.Cl.Cl.CCOCC1(CCC(CC1)C2=N[NH]C=C2CN(C)CCNC)COCC

Mechanism of Action

Targets/IC₅₀/Ki	PRMT1 PRMT3 PRMT4 PRMT6 PRMT8
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.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/31257072/

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