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GSK126 [1346574-57-9]

Imprimer

Référence HY-13470-5mg

Conditionnement : 5mg

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Description

GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM^[1].

IC₅₀ & Target^[1]

EZH2

9.9 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	10.4 μM Compound: GSK126	Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against mouse 4T1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A2780	IC₅₀	12 μM Compound: GSK126	Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A549	GI₅₀	18.7 μM Compound: GSK-126	Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
A549	IC₅₀	23 μM Compound: GSK126	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
A549	IC₅₀	23.65 nM Compound: Chemical probe: GSK126	Antiproliferative activity against human A549 cells harbouring KrasG12D/+ mutant assessed as reduced cell viability treated for 96 hrs in RPMI medium by cell titre blue reagent based assay (Rvb = 32.03 nM) Antiproliferative activity against human A549 cells harbouring KrasG12D/+ mutant assessed as reduced cell viability treated for 96 hrs in RPMI medium by cell titre blue reagent based assay (Rvb = 32.03 nM)	[PMID: 30487290]
A549	IC₅₀	6.9 nM Compound: Chemical probe: GSK126	Antiproliferative activity against human A549 cells harbouring KrasG12D/+ mutant assessed as reduced cell viability treated for 96 hrs in IFN medium by cell titre blue reagent based assay (Rvb = 8.1 nM) Antiproliferative activity against human A549 cells harbouring KrasG12D/+ mutant assessed as reduced cell viability treated for 96 hrs in IFN medium by cell titre blue reagent based assay (Rvb = 8.1 nM)	[PMID: 30487290]
BT-549	IC₅₀	16.27 μM Compound: GSK126	Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
BT-549	IC₅₀	19.19 μM Compound: GSK; GSK126	Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay Cytotoxicity against human BT-549 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
BT-549	IC₅₀	23.3 μM Compound: GSK126	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
BT-549	IC₅₀	8.28 μM Compound: GSK; GSK126	Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human BT-549 cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
Daudi	GI₅₀	11.2 μM Compound: GSK-126	Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human Daudi cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
ES-2	IC₅₀	32.2 μM Compound: GSK126	Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human ES2 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
HeLa	IC₅₀	0.28 μM Compound: GSK-126	Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 levels incubated for 72 hrs by ELISA method	[PMID: 26189078]
HEY	IC₅₀	>100 μM Compound: GSK126	Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human HEY cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
HK-2	IC₅₀	>40 μM Compound: GSK126	Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HK-2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
HL-60	IC₅₀	14.05 μM Compound: GSK126	Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
L02	IC₅₀	>40 μM Compound: GSK126	Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF-10A	IC₅₀	>40 μM Compound: GSK126	Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF-10A cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MCF-10A	IC₅₀	>40 μM Compound: GSK; GSK126	Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MCF-10A	IC₅₀	>40 μM Compound: GSK; GSK126	Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human MCF-10A cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
MCF7	IC₅₀	18.8 μM Compound: GSK126	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
MCF7	IC₅₀	21.38 μM Compound: GSK126	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-231	IC₅₀	12.82 μM Compound: GSK126	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
MDA-MB-231	IC₅₀	13.18 μM Compound: GSK; GSK126	Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs by MTT assay	[PMID: 38134746]
MDA-MB-231	IC₅₀	6.32 μM Compound: GSK; GSK126	Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Niraparib by MTT assay Synergistic cytotoxicity against human MDA-MB-231 cells incubated for 72 hrs in presence of Niraparib by MTT assay	[PMID: 38134746]
MDA-MB-468	IC₅₀	11.92 μM Compound: GSK126	Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
Medulloblastoma cell	IC₅₀	4.64 μM Compound: Chemical Probe: GSK126	Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay Antiproliferative activity in Ptch1-deficient mouse medulloblastoma cell after 48 hrs by CCK-8 assay	[PMID: 32579914]
MV4-11	IC₅₀	7.34 μM Compound: GSK126	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 35623249]
NCI-H1703	IC₅₀	>100 μM Compound: GSK126	Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1703 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OAW-42	IC₅₀	55.4 μM Compound: GSK126	Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OAW-42 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
OVCAR-3	IC₅₀	29.8 μM Compound: GSK126	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PA-1	IC₅₀	12.2 μM Compound: GSK126	Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human PA-1 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
PC-3	GI₅₀	9.4 μM Compound: GSK-126	Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
PC-3	IC₅₀	10.04 μM Compound: 8; GSK126	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay	[PMID: 35569264]
Pfeiffer	GI₅₀	0.18 μM Compound: GSK-126	Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human Pfeiffer cells expressing EZH2 A667G mutant assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
SK-BR-3	IC₅₀	15.5 μM Compound: GSK126	Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
SK-OV-3	IC₅₀	10.49 μM Compound: 8; GSK126	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 3 to 7 days followed by replacement of medium containing compound every 3 days by CCK8 assay	[PMID: 35569264]
SK-OV-3	IC₅₀	68.4 μM Compound: GSK126	Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 36692394]
T98G	GI₅₀	12.6 μM Compound: GSK-126	Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human T98G cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
U2932	GI₅₀	6.7 μM Compound: GSK-126	Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human U2932 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]
U-87MG ATCC	GI₅₀	28.5 μM Compound: GSK-126	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24767850]

In Vitro

GSK126 potently inhibits both wild-type and mutant EZH2 methyltransferase activity with similar potencies (K_i=0.5-3 nM) independent of substrate used, and is competitive with S-adenosyl-methionine (SAM) and non-competitive with peptide substrates. GSK126 is highly selective against other methyltransferases and multiple other protein classes (EZH1, IC₅₀=680 nM)^[1]. Treatment of three SCLC cell lines with GSK126, induces growth inhibition. SCLC cell lines (Lu130, H209, and DMS53) are treated with 0.5, 2, and 8 μM GSK126, and growth curve is analyzed by WST-8 assay. Inhibition of cellular growth by GSK126 treatment is observed at 8 μM in all the three cell lines, while Lu130 and H209 are more sensitive to GSK126, even at lower doses^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : 12.5 mg/mL (23.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8987 mL	9.4936 mL	18.9872 mL
5 mM	0.3797 mL	1.8987 mL	3.7974 mL
10 mM	0.1899 mL	0.9494 mL	1.8987 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.37 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1.25 mg/mL (2.37 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (2.37 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.82 mg/mL (1.56 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (18.99 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 1% CMC/0.5% Tween-80 in Saline water
Solubility: 10 mg/mL (18.99 mM); Suspended solution; Need ultrasonic

Pureté et documentation

Purity: 99.98%

Fiche technique (284 KB) SDS (537 KB)

COA (256 KB) HNMR (213 KB) RP-HPLC (148 KB) LCMS (122 KB)

Instruction de manipulation (2659 KB)

Références

[1]. McCabe MT, et al. EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations. Nature. 2012 Dec 6;492(7427):108-12. [Content Brief]

[2]. Sato T, et al. PRC2 overexpression and PRC2-target gene repression relating to poorer prognosis in small cell lung cancer. Sci Rep. 2013 May 29;3:1911. [Content Brief]

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GSK126 [1346574-57-9]

Référence HY-13470-5mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

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