EZH1/2

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S7004	EPZ005687	<1 mg/mL	2 mg/mL	<1 mg/mL
S7164	GSK343	<1 mg/mL	1 mg/mL	4 mg/mL
S7128	Tazemetostat (EPZ-6438)	<1 mg/mL	5 mg/mL	<1 mg/mL
S7165	UNC1999	<1 mg/mL	20 mg/mL	50 mg/mL
S8702	EBI-2511	<1 mg/mL	30 mg/mL	13 mg/mL
S8353	CPI-1205	<1 mg/mL	100 mg/mL	100 mg/mL
S7805	EPZ011989	<1 mg/mL	<1 mg/mL	100 mg/mL
S8494	PF-06726304	<1 mg/mL	10 mg/mL	22 mg/mL
S7611	EI1	<1 mg/mL	42 mg/mL	<1 mg/mL
S7804	GSK503	<1 mg/mL	100 mg/mL	26 mg/mL
S7061	GSK126	<1 mg/mL	3 mg/mL	<1 mg/mL
S7656	CPI-360	<1 mg/mL	20 mg/mL	18 mg/mL
S7616	CPI-169	<1 mg/mL	100 mg/mL	100 mg/mL

EZH1/2 Products

All (14) EZH1/2 Inhibitors (14) New EZH1/2 Products

Catalog No.	Information	Product Use Citations	Product Validations
S7004	EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2 with K_i of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Biol Chem, 2017, pii: jbc.M116.765800	Representative images of OPCs treated for 72 h with the indicated EZH2 inhibitors. All treatments are at 2 μM. Scale bar, 100 μm.
S7164	GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.	Nucleic Acids Res, 2016, 44(16):7659-72 Mol Cancer, 2017, 16(1):5 Oncogene, 2015, 10.1038/onc.2015.38	Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
S7128	Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with K_i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.	Nature, 2018, 560(7718):372-376 Cell, 2018, 175(1):186-199 J Pathol, 2017, 242(3):371-383	EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
S7165	UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Pathol, 2018, 245(4):433-444	Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.
S8702^New	EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
S8353	CPI-1205 CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
S7805	EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with K_i of <3 nM.	J Cancer, 2018, 9(20):3787-3796
S8494	PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
S7611	EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.	Mol Cancer, 2017, 10.1186/s12943-016-0575-6 Oncotarget, 2015, 6(32):32410-25	EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors.
S7804	GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.	J Pathol, 2018, 245(4):433-444 Front Immunol, 2016, 7:496	LC3B‐II levels are increased following 120 h treatment of GSK503 (G, CRMM1 and CRMM2 at 10 μm, and CM2005.1 at 15 μm) or UNC1999 (U, 6 μm).
S7061	GSK126 GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.	Nature, 2019, 566(7743):270-274 Nature, 2019, 566(7744):344-349 Mol Cancer, 2017, 16(1):22	HeLa cells were transfected with NS (nonspecific) or EZH2-specific siRNA for 48 h with protease inhibitors (10 μM E64 and 10 μM pepstatin-A). Cells were stained with LC3B antibody (green) and DAPI, and observed under confocal microscopy for LC3B puncta. Scale bars: 10 μm
S7656	CPI-360 CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
S7616	CPI-169 CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

Catalog No.	Information	Product Use Citations	Product Validations
S7004	EPZ005687 EPZ005687 is a potent and selective inhibitor of EZH2 with K_i of 24 nM in a cell-free assay, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Biol Chem, 2017, pii: jbc.M116.765800	Representative images of OPCs treated for 72 h with the indicated EZH2 inhibitors. All treatments are at 2 μM. Scale bar, 100 μm.
S7164	GSK343 GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.	Nucleic Acids Res, 2016, 44(16):7659-72 Mol Cancer, 2017, 16(1):5 Oncogene, 2015, 10.1038/onc.2015.38	Representative confocal microscopy images of oocytes with DZNep or GSK343 treatment. The oocytes presented with a typical barrel-shaped spindle and well-aligned chromosomes on the metaphase plate not only in DZNep or GSK343 treated group but also in the control group. Spindle was recognized by α-tubulin (green) and DNA was recognized by PI (Propidium iodide, red). Scale bar = 4 μm.
S7128	Tazemetostat (EPZ-6438) Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with K_i and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.	Nature, 2018, 560(7718):372-376 Cell, 2018, 175(1):186-199 J Pathol, 2017, 242(3):371-383	EZH2i-induced H3K27ac level change in cancer cells. Cells were treated with 1 mM EPZ-6438 and 1 mM GSK126 for 6 days, respectively. H3K27ac was detected by immunoblotting. Lysates from each cell line were blotted individually. EPZ: EPZ-6438.
S7165	UNC1999 UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM in cell-free assays, respectively, showing >1000-fold selectivity over a broad range of epigenetic and non-epigenetic targets.	Nature, 2018, 560(7718):372-376 Oncogene, 2015, 10.1038/onc.2015.38 J Pathol, 2018, 245(4):433-444	Ex vivo growth of the SCLC PDX LX92 is significantly inhibited by the EZH2 inhibitors EPZ-5687, GSK343 and UNC1999 as measured by resazurin conversion (two-way analysis of variance, adjusted for multiple comparisons by the method of Dunnet).
S8607	JQ-EZ-05 (JQEZ5) JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.
S8702^New	EBI-2511 EBI-2511 is a highly potent and orally active EZH2 inhibitor with an IC50 of 4 nM for EZH2(A667G).
S8353	CPI-1205 CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
S7805	EPZ011989 EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with K_i of <3 nM.	J Cancer, 2018, 9(20):3787-3796
S8494	PF-06726304 PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
S7611	EI1 EI1 is a potent and selective EZH2 inhibitor with IC50 of 15 nM and 13 nM for EZH2 (WT) and EZH2 (Y641F), respectively.	Mol Cancer, 2017, 10.1186/s12943-016-0575-6 Oncotarget, 2015, 6(32):32410-25	EZH2 inhibitors EI1 or GSK343 are applied in MDA-MB-231 breast cancer cells with NBAT1 over-expression. The invasion suppression effects of NBAT1 was reversed by concomitant EZH2 inhibitors.
S7804	GSK503 GSK503 is a potent and specific EZH2 methyltransferase inhibitor.	J Pathol, 2018, 245(4):433-444 Front Immunol, 2016, 7:496	LC3B‐II levels are increased following 120 h treatment of GSK503 (G, CRMM1 and CRMM2 at 10 μm, and CM2005.1 at 15 μm) or UNC1999 (U, 6 μm).
S7061	GSK126 GSK126 is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.	Nature, 2019, 566(7743):270-274 Nature, 2019, 566(7744):344-349 Mol Cancer, 2017, 16(1):22	HeLa cells were transfected with NS (nonspecific) or EZH2-specific siRNA for 48 h with protease inhibitors (10 μM E64 and 10 μM pepstatin-A). Cells were stained with LC3B antibody (green) and DAPI, and observed under confocal microscopy for LC3B puncta. Scale bars: 10 μm
S7656	CPI-360 CPI-360 is a potent, selective,and SAM-competitive EZH1 inhibitor with IC50 of 102.3 nM, >100-fold selectivity over other methyltransferases.
S7616	CPI-169 CPI-169 is a potent, and selective EZH2 inhibitor with IC50 of 0.24 nM, 0.51 nM, and 6.1 nM for EZH2 WT, EZH2 Y641N, and EZH1, respectively.

Tags: EZH1/2 inhibitors | EZH1/2 modulators | EZH1/2 chemical | EZH1/2 Inhibition

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