GSK126 (Synonyms: GSK2816126A)

Name: GSK126
Brand: MedChemExpress
SKU: HY-13470
Rating: 5.0 (98 reviews)

Cat. No.: HY-13470 Purity: 99.75%: Data Sheet
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GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC₅₀ of 9.9 nM.

For research use only. We do not sell to patients.

CAS No. : 1346574-57-9

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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Based on 98 publication(s) in Google Scholar

98 Publications Citing Use of MCE GSK126

: GSK126 purchased from MedChemExpress. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19. [Abstract]; Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.

: GSK126 purchased from MedChemExpress. Usage Cited in: J Exp Med. 2018 May 7;215(5):1365-1382. [Abstract]; Immunoblot analysis of Ezh2, H3K27me3, H3, and Hsp60 (loading control) in whole-cell lysates of the indicated proinflammatory genes of macrophages or microglia that are pretreated with DMSO or GSK126 (4 μM) for 3 d and then left nontreated (NT) or stimulated for 6 h with the ligands of different TLRs.

: GSK126 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]; The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

: GSK126 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Sep 29;6(29):27023-36. [Abstract]; This includes ATF3 (Activating Transcription Factor 3) and metastasis suppressor NDRG1 (N-Myc Downstream Regulated Gene 1) that also shows an upregulation in protein expression (phosphorylated at threonine 346) with GSK126 in two EZH2 mutant cell lines by western blot.

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms

EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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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 3 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]
A549	GI₅₀	18.7 3 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]
4T1	IC₅₀	10.4 3 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 3 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]
BT-549	IC₅₀	16.27 3 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]
A2780	IC₅₀	12 3 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 3 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]
Daudi	GI₅₀	11.2 3 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]
A549	GI₅₀	18.7 3 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 3 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]
HeLa	IC₅₀	0.28 3 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]
A549	IC₅₀	23 3 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]
BT-549	IC₅₀	16.27 3 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]
A549	IC₅₀	23.65 1 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]
HK-2	IC₅₀	> 40 3 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]
BT-549	IC₅₀	23.3 3 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]
A549	IC₅₀	6.9 1 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]
HL-60	IC₅₀	14.05 3 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]
BT-549	IC₅₀	16.27 3 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]
Daudi	GI₅₀	11.2 3 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]
L02	IC₅₀	> 40 3 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]
BT-549	IC₅₀	19.19 3 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]
MCF-10A	IC₅₀	> 40 3 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]
ES-2	IC₅₀	32.2 3 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]
BT-549	IC₅₀	23.3 3 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]
MCF7	IC₅₀	21.38 3 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]
HeLa	IC₅₀	0.28 3 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]
BT-549	IC₅₀	8.28 3 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]
MDA-MB-231	IC₅₀	12.82 3 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]
HEY	IC₅₀	>100 3 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]
MDA-MB-468	IC₅₀	11.92 3 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]
HK-2	IC₅₀	>40 3 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]
Daudi	GI₅₀	11.2 3 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]
MV4-11	IC₅₀	7.34 3 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]
HL-60	IC₅₀	14.05 3 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 3 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]
ES-2	IC₅₀	32.2 3 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]
PC-3	IC₅₀	10.04 3 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]
HEY	IC₅₀	> 100 3 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]
PC-3	GI₅₀	9.4 3 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]
MCF-10A	IC₅₀	>40 3 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]
MCF7	IC₅₀	21.38 3 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]
HK-2	IC₅₀	> 40 3 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]
Pfeiffer	GI₅₀	0.18 3 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-OV-3	IC₅₀	10.49 3 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]
MCF7	IC₅₀	18.8 3 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]
HL-60	IC₅₀	14.05 3 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]
HeLa	IC₅₀	0.28 3 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]
T98G	GI₅₀	12.6 3 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]
MDA-MB-231	IC₅₀	12.82 3 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]
U2932	GI₅₀	6.7 3 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]
MDA-MB-468	IC₅₀	11.92 3 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]
U-87MG ATCC	GI₅₀	28.5 3 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]
MV4-11	IC₅₀	7.34 3 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]
L02	IC₅₀	> 40 3 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]
NCI-H1703	IC₅₀	>100 3 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]
MCF-10A	IC₅₀	> 40 3 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 3 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]
OAW-42	IC₅₀	55.4 3 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]
MCF-10A	IC₅₀	> 40 3 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]
OVCAR-3	IC₅₀	29.8 3 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]
MCF7	IC₅₀	18.8 3 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]
PA-1	IC₅₀	12.2 3 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]
MCF7	IC₅₀	21.38 3 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]
PC-3	GI₅₀	9.4 3 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]
MDA-MB-231	IC₅₀	12.82 3 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]
PC-3	IC₅₀	10.04 3 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]
MDA-MB-231	IC₅₀	13.18 3 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]
Pfeiffer	GI₅₀	0.18 3 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]
MDA-MB-231	IC₅₀	6.32 3 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]
SK-BR-3	IC₅₀	15.5 3 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 3 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 3 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]
MDA-MB-468	IC₅₀	11.92 3 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]
MV4-11	IC₅₀	7.34 3 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]
T98G	GI₅₀	12.6 3 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]
Medulloblastoma cell	IC₅₀	4.64 3 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]
U2932	GI₅₀	6.7 3 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]
NCI-H1703	IC₅₀	> 100 3 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]
U-87MG ATCC	GI₅₀	28.5 3 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]
OAW-42	IC₅₀	55.4 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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 3 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]
U-87MG ATCC	GI₅₀	28.5 3 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]
U2932	GI₅₀	6.7 3 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]

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.

In Vivo

GSK126 is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight in female beige SCID mice. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice^[1].

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

Molecular Weight

526.67

Formula

C₃₁H₃₈N₆O₂

CAS No.

1346574-57-9

Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CC(C2=CC=C(N3CCNCC3)N=C2)=CC4=C1C(C)=CN4[C@@H](C)CC)NCC5=C(C)C=C(C)NC5=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (284 KB) SDS (537 KB)

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

Handling Instructions (2659 KB)

References

[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]

Kinase Assay ^[1]	The five-member PRC2 complex (Flag-EZH2, EED, SUZ12, AEBP2, RbAp48) containing either wild-type or mutant (A677G, Y641N, Y641C, Y641H, Y641S or Y641F) EZH2 is prepared. GSK126 is dissolved in DMSO and tested at concentrations of 0.6 nM to 300 nM with a final DMSO concentration of 2.5%. In contrast to wild-type EZH2 which prefers H3K27me0 as a substrate in vitro, EZH2 Y641 mutants prefer H3K27me2 and have little activity with H3K27me0 or H3K27me1. The A677G mutant is distinct from both the wild-type and Y641 mutant forms of EZH2 in that it efficiently methylates H3K27me0, H3K27me1, and H3K27me2; therefore, histone H3 peptides (residues 21-44; 10 μM final) with either K27me0 (wild type, A677G EZH2), K27me1 (A677G EZH2), or K27me2 (A677G, Y641N, Y641C, Y641H, Y641S and Y641F EZH2) are used as methyltransferase substrates. GSK126 is added to plates followed by addition of 6 nM EZH2 complex and peptide. As the potency of GSK126 is at or near the tight binding limit of an assay run at [SAM]=K_m, _IC50 values are measured at a high concentration of the competitive substrate SAM relative to its K_m (7.5 μM SAM where the SAM K_m is 0.3 μM)^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[2]	JUB- and PTRF-introduced DMS53 cells are seeded at density of 1×10³ cells/well in 96-well plate, and cellular growth is analyzed using WST-8 kit at 12, 36, 60, and 84 h. Cellular growth of Lu130, H209, and DMS53 with treatment by DZNep or GSK126 is also analyzed using WST-8 kit. DZNep is dissolved in PBS at 5 mM, and cells are cultured at the final concentration of 5 μM. GSK126 is dissolved in DMSO at 10 mM, and cells are cultured at 0.5, 2, and 8 μM^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] GSK126 or vehicle is administered intraperitoneally at a dose volume of 0.2 mL per 20 g body weight. Pfeiffer or KARPAS-422 cells (1×10⁷) in 100% Matrigel are implanted subcutaneously in female beige SCID mice. Tumors are measured with calipers, and block randomized according to tumour size into treatment groups. For efficacy studies, 10 mice are randomized in each treatment group before the initiation of dosing and GSK126 treatment is initiated once the tumour volumes are approximately 200 mm³ in the Pfeiffer and KARPAS-422 studies and 500 mm³ in the KARPAS-422 intermittent dosing study. Mice are weighed and tumors measured with calipers twice weekly. Two-tailed t-tests are conducted assuming two samples of equal variance. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8987 mL	9.4936 mL	18.9872 mL	47.4681 mL
	5 mM	0.3797 mL	1.8987 mL	3.7974 mL	9.4936 mL
	10 mM	0.1899 mL	0.9494 mL	1.8987 mL	4.7468 mL
	15 mM	0.1266 mL	0.6329 mL	1.2658 mL	3.1645 mL
	20 mM	0.0949 mL	0.4747 mL	0.9494 mL	2.3734 mL

GSK126 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK1261346574-57-9GSK2816126AGSK 126GSK-126Histone MethyltransferaseInhibitorinhibitorinhibit

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GSK126 (Synonyms: GSK2816126A)

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