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GSK126 EZH2 inhibitor

Cat.No.S7061

GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.

GSK126 EZH2 inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 526.67

Quality Control

Batch: Purity: 99.91%

99.91

Related Targets	HDAC JAK BET Histone Methyltransferase PKC PARP HIF PRMT AMPK Sirtuin
Other EZH2 Inhibitors	PF-06821497 Tulmimetostat (CPI-0209) Valemetostat (DS-3201) GSK343 Lirametostat (CPI-1205) CPI-169 MS1943 SHR2554 EZH2/HSP90-IN-29 EBI-2511

Solubility in DMSO or Water

In vitro
Batch:

DMSO : 5 mg/mL (9.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 14 mg/mL (26.58 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 10 mg/mL (18.98 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 10 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 12 mg/mL (22.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

The solubility data above are all experimental results (not literature values).

DMSO : 16 mg/mL (30.37 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

The solubility data above are all experimental results (not literature values).

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.
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	4%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.95mM)	Taking the 1 mL working solution as an example, add 40 μL of 12.5 mg/ml clear DMSO stock solution to 960 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
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.
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.
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.

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.

Read more about GSK126 solubility in DMSO or water

Working Concentrations for Cell Culture Treatment

Read more about GSK126 working concentrations for cell culture treatment

Working Concentrations for Animal Model Treatment

Mechanism of Action

Information	GSK126 is a highly selective EZH2 inhibitor. It affects Rho/ROCK, Notch, and AMPK/PPAR-γ signaling by decreasing H3K27me3 levels to modulate epigenetic transcription, effectively inhibiting tumor proliferation and fibrosis, while promoting apoptosis.
Read more about GSK126 IC50 for cell-based and cell-free assays
Primary Applications and Mechanism of Action

Read more about GSK126 Mechanism of Action

Chemical Information, Storage & Stability

Molecular Weight	526.67	Formula	C₃₁H₃₈N₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1346574-57-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GSK2816126A, GSK2816126			Smiles	CCC(C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NCC5=C(C=C(NC5=O)C)C)C

Read more about storage & stability

GSK126 Combination Database

Read more comparative analysis about GSK126

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Could you please suggest a vehicle for in vivo uses of this compound without oil?

Answer:
It could be dissolved in 4% DMSO+30% PEG 300+ddH2O (0.5mg/ml).

Question 2:
Does this compound require an activation step to be functional? For example, an acidic or basic environment.

Answer:
It does not require an activation step to be functional.

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions

Concentration (start):

Dilution-folds:

Computed Result

C1=C0/X	C1:		LOG(C1):
C2=C1/X	C2:		LOG(C2):
C3=C2/X	C3:		LOG(C3):
C4=C3/X	C4:		LOG(C4):
C5=C4/X	C5:		LOG(C5):
C6=C5/X	C6:		LOG(C6):
C7=C6/X	C7:		LOG(C7):
C8=C7/X	C8:		LOG(C8):