EZH1/2
抑制剂选择性比较
EZH1/2产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7004 |
EPZ005687EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。 |
Representative images of OPCs treated for 72 h with the indicated EZH2 inhibitors. All treatments are at 2 μM. Scale bar, 100 μm.
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| S7164 |
GSK343GSK343是一种有效的，选择性EZH2抑制剂，无细胞试验中IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。 |
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.
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| S7128 |
Tazemetostat (EPZ-6438)Tazemetostat (EPZ-6438)是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。 |
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.
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| S7165 |
UNC1999UNC1999一种有效的具有口服活性的EZH2和EZH1选择性抑制剂，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。 |
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).
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| S8607 |
JQ-EZ-05 (JQEZ5)JQ-EZ-05是可逆的、特异的EZH1/2抑制剂。 |
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| S8702New |
EBI-2511EBI-2511是一种有效的、具有口服活性的EZH2抑制剂，对EZH2(A667G)的IC50值为4 nM。 |
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| S8353 |
CPI-1205CPI-1205是具有口服生物活性的选择性组蛋白赖氨酸甲基转移酶EZH2的抑制剂，对EZH2和EZH1的IC50分别为2 nM和52 nM。它具有潜在的抗肿瘤活性。 |
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| S7805 |
EPZ011989EPZ011989是一种有效的、选择性的、具有口服活性的EZH2抑制剂，Ki值<3 nM。 |
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| S8494 |
PF-06726304PF-06726304是选择性EZH2抑制剂，对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。 |
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| S7611 |
EI1EI1是一种有效的选择性EZH2抑制剂，对EZH2 (WT)和EZH2 (Y641F)的IC50分别为15 nM和13 nM。 |
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. |
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| S7804 |
GSK503GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。 |
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).
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| S7061 |
GSK126GSK126 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。 |
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.
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| S7656 |
CPI-360CPI-360是一种有效的，选择性的，且SAM竞争性EZH1抑制剂，IC50为102.3 nM，选择性比作用于其它甲基转移酶高100多倍。 |
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| S7616 |
CPI-169CPI-169是一种有效的选择性EZH2抑制剂，作用于EZH2 WT，EZH2 Y641N，和EZH1的IC50分别为0.24 nM，0.51 nM，和6.1 nM。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S7004 |
EPZ005687EPZ005687是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki为24 nM，比作用于EZH1选择性高50倍，比作用于15种其他蛋白甲基转移酶选择性高500倍。 |
Representative images of OPCs treated for 72 h with the indicated EZH2 inhibitors. All treatments are at 2 μM. Scale bar, 100 μm.
|
|
| S7164 |
GSK343GSK343是一种有效的，选择性EZH2抑制剂，无细胞试验中IC50为4 nM，比作用于EZH1选择性高60倍，比作用于其他组蛋白甲基转移酶选择性高1000倍以上。 |
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)是一种有效的，选择性EZH2抑制剂，无细胞试验中Ki 和 IC50分别为2.5 nM 和 11 nM，比作用于EZH1选择性高35倍，比作用于14种其他HMT选择性高4500多倍。 |
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 |
UNC1999UNC1999一种有效的具有口服活性的EZH2和EZH1选择性抑制剂，无细胞试验中IC50分别为2 nM和45 nM，对广泛表观遗传学相关或不相关的靶点选择性大于1000倍。 |
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是可逆的、特异的EZH1/2抑制剂。 |
||
| S8702New |
EBI-2511EBI-2511是一种有效的、具有口服活性的EZH2抑制剂，对EZH2(A667G)的IC50值为4 nM。 |
||
| S8353 |
CPI-1205CPI-1205是具有口服生物活性的选择性组蛋白赖氨酸甲基转移酶EZH2的抑制剂，对EZH2和EZH1的IC50分别为2 nM和52 nM。它具有潜在的抗肿瘤活性。 |
||
| S7805 |
EPZ011989EPZ011989是一种有效的、选择性的、具有口服活性的EZH2抑制剂，Ki值<3 nM。 |
||
| S8494 |
PF-06726304PF-06726304是选择性EZH2抑制剂，对WT EZH2和EZH2(Y641N)的Ki值分别为0.7 nM和3 nM。抑制H3K27me3的IC50为15 nM。 |
||
| S7611 |
EI1EI1是一种有效的选择性EZH2抑制剂，对EZH2 (WT)和EZH2 (Y641F)的IC50分别为15 nM和13 nM。 |
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 |
GSK503GSK503是一种有效的特异性EZH2甲基转移酶抑制剂。 |
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 |
GSK126GSK126 是一种有效的，高选择性EZH2 methyltransferase抑制剂，IC50为9.9 nM，对 EZH2 的选择性比其他20种人甲基转移酶高1000多倍。 |
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-360CPI-360是一种有效的，选择性的，且SAM竞争性EZH1抑制剂，IC50为102.3 nM，选择性比作用于其它甲基转移酶高100多倍。 |
||
| S7616 |
CPI-169CPI-169是一种有效的选择性EZH2抑制剂，作用于EZH2 WT，EZH2 Y641N，和EZH1的IC50分别为0.24 nM，0.51 nM，和6.1 nM。 |
