Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1788 |
Tazemetostat
E-7438,EPZ6438 |
Histone Methyltransferase | Chromatin/Epigenetic |
Tazemetostat (EPZ6438) 是一种组蛋白甲基转移酶 EZH2 抑制剂 (IC50=11 nM),具有口服活性、选择性和 SAM 竞争性。Tazemetostat 具有抗肿瘤活性,可以用于治疗上皮样肉瘤/滤泡性淋巴瘤。 | |||
T17002 |
Tazemetostat hydrobromide
E-7438 hydrobromide,氢溴酸泰泽司他,EPZ-6438 hydrobromide |
Histone Methyltransferase | Chromatin/Epigenetic |
Tazemetostat hydrobromide (E-7438 hydrobromide) 是口服的EZH2选择性抑制剂。它抑制含有 PRC2 复合体的野生型 EZH2 的活性,Ki 为 2.5 nM。它还抑制 EZH1,IC50为 392 nM。 | |||
T3057 |
UNC1999
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
UNC1999 是一种可口服的,选择性和 SAM-竞争性的 EZH2和 EZH1抑制剂,IC50分别为 <10 nM 和 45 nM。 | |||
T2435 |
EPZ011989
|
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ011989是一种高选择性可口服的 EZH2抑制剂,对wt EZH2以及EZH2突变型Ki 值<3nM。 | |||
T13279L |
Valemetostat
DS-3201 |
Histone Methyltransferase | Chromatin/Epigenetic |
Valemetostat (DS-3201) 是一种EZH1/2抑制剂,可用于研究复发/难治性周围 T 细胞淋巴瘤。 | |||
T6809 |
CPI-169 racemate
CPI 169,CPI-169,CPI169 |
Epigenetic Reader Domain; Histone Methyltransferase | Chromatin/Epigenetic |
CPI-169 racemate (CPI 169) 是CPI-169的消旋体。CPI-169 是一种有效的选择性 EZH2 抑制剂,对 EZH2 WT、EZH2 Y641N 和 EZH1 的 IC50 分别为 0.24、0.51 和 6.1 nM。 | |||
T6059 |
GSK343
|
Histone Methyltransferase; Autophagy | Autophagy; Chromatin/Epigenetic |
GSK343 是一种特异性且有效的 EZH2 抑制剂,IC50为 4 nM。它对 EZH1 的特异性活性是 60 倍。 | |||
T40199 |
Tulmimetostat
CPI-0209 |
Histone Methyltransferase | Chromatin/Epigenetic |
Tulmimetostat (CPI-0209) 是一种具有口服活性的 EZH1/EZH2 抑制剂。Tulmimetostat 有抗肿瘤活性,用于研究卵巢癌和晚期实体瘤。 | |||
T1905 |
EPZ005687
|
Histone Methyltransferase | Chromatin/Epigenetic |
EPZ005687 是一种选择性EZH2抑制剂,Ki 值为 24 nM,对其选择性是对 EZH1 的 50 倍,对其他 15 种甲基转移酶的 500 倍。 | |||
T6810 |
CPI-360
Synonym 2,CPI 360,CPI360 |
Apoptosis; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
CPI-360是一种小分子EZH2抑制剂(IC50:0.002 μM,EC50: 0.080μM),在EZH200依赖性肿瘤异种移植模型中显示出抗肿瘤活性。 | |||
T13279 |
Valemetostat tosylate
DS-3201 tosylate |
Histone Methyltransferase | Chromatin/Epigenetic |
Valemetostat tosylate is a dual inhibitor of EZH1/2 and used in the research of relapsed/refractory peripheral T-cell lymphoma. | |||
T25400 |
EZH2-IN-3
EZH2 inhibitor 3,EZH2-inhibitor-3 |
||
EZH2-IN-3 is an inhibitor of EZH2 and EZH1 with selective impact on diffuse large B cell lymphoma cell growth. | |||
T23575 |
(R)-OR-S1
(R)ORS1,(R) OR S1,R-OR-S1 |
||
(R)-OR-S1 is a SAM-competitive, highly selective, orally bioavailable dual inhibitor of EZH1/2. | |||
T73134 | EZH2-IN-14 | ||
EZH2-IN-14为一种选择性EZH2(Histone Methyltransferase)抑制剂,具IC50值12 nM。该化合物通过抑制EZH2/PRC2的甲基转移酶活性(减少H3K27me3),显著抑制其功能。相比高度同源的H3K27甲基转移酶EZH1,EZH2-IN-14对EZH2的选择性提高200倍以上。 | |||
T73115 |
(S)-HH2853
|
||
(S)-HH2853 是一种 PYRIDINO 五元芳环化合物,一种有效的 EZH1/2双重抑制剂,对 EZH2_Y641F 的IC50为 <100 nM。(S)-HH2853有潜力用于抗肿瘤或自身免疫性疾病的研究。 | |||
T27069 |
CPI-169
CPI 169 (R),CPI-169 (R) |
||
CPI-169 (R) is a novel and potent inhibitor of EZH2. | |||
T2435L |
EPZ011989 HCl(1598383-40-4 Free base)
EPZ-011989 TFA,EPZ011989 TFA salt,EPZ 011989 TFA,EPZ011989 TFA |
||
EPZ011989为一高效选择性口服EZH2抑制剂,Ki值<3 nM。 | |||
T15240 |
Tazemetostat trihydrochloride
EPZ-6438 trihydrochloride,E-7438 trihydrochloride |
Histone Methyltransferase | Chromatin/Epigenetic |
Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo |