所有图片(1)
Ezh2/Ezh1 Inhibitor, UNC1999, Enhancer of Zested Homolog 1 Inhibitor, 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide, Ezh1 Inhibitor, Ezh2 Inhibitor IV, HMTase Inhibitor XII, Histone Lysi, Enhancer of Zested Homolog 1 Inhibitor, 1-Isopropyl-6-(6-(4-isopropylpiperazin-1-yl)pyridin-3-yl)-N-((6-methyl-2-oxo-4-propyl-1,2-dihydropyridin-3-yl)methyl)-1H-indazole-4-carboxamide, Ezh1 Inhibitor, Ezh2 Inhibitor IV, HMTase Inhibitor XII, Histone Lysin
C33H43N7O2
推荐产品
检测方案
≥98% (HPLC)
质量水平
形式
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 100 mg/mL
储存温度
2-8°C
SMILES字符串
CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C
一般描述
A cell-permeable GSK126 structural analog that acts as a potent, SAM-, but not substrate-, competitive inhibitor against Ezh1 and Ezh2 (IC50 = 5 and 45 nM against PRC2 complex containing Ezh2 or Ezh1 in H3 peptide methylation assays; [SAM] = 5 µM), while exhibiting much reduced or little potency toward panels of 15 other methyltransferases, 50 kinases, as well as 43 GPCRs, transporters, and ion channels, although high affinity binding is observed with Sigma-2 receptor S2R/PGRMC1 (Ki = 65 nM) with unknown impact toward its function. Cellular H3K27me3 level is shown to be largely reduced in MCF10A, MCF7, and DB cells with no significant effect on proliferation upon a 3-day UNC1999 treatment (ICmax = 3 to 5 µM), while complete cell death is reported in the EZH2 Y641N-harboring DB cell line upon an 8-day 5 µM drug exposure. Both its oral bioavailability in mice and enhanced Ezh1 potency can greatly complement the Ezh2-selective GSK126 in in vitro and in vivo studies.
A cell-permeable GSK126 structural analog that acts as a potent, SAM-, but not substrate-, competitive inhibitor against Ezh1 and Ezh2 (IC50 = 5, 20, 20, 45 nM against PRC2 complex containing Ezh2 wt, Ezh2 Y641F, Ezh2 Y641N, or wt Ezh1 in H3 peptide methylation assays; [SAM] = 5 µM), while exhibiting much reduced or little potency toward panels of 15 other methyltransferases (IC50 >10 µM), 50 kinases (≤20% inhibition at 10µM), as well as 43 GPCRs, transporters, and ion channels, although high affinity binding is observed with Sigma-2 receptor S2R/PGRMC1 (Ki = 65 nM) with unknown impact toward its function. Cellular H3K27me3 level is shown to be largely reduced in MCF10A, MCF7, and DB cells with no significant effect on proliferation upon a 3-day UNC1999 treatment (ICmax = 3 to 5 µM), while complete cell death is reported in the EZH2 Y641N-harboring DLBCL line DB cell culture upon an 8-day 5 µM drug exposure. Exhibits good bioavailability in mice with the plasma drug concentration maintained above 100 nM for 20 h and 24 h, respectively, following a single 50 mg/kg oral or i.p. dosage (Cmax = 4.7 and >9.7 µM, respectively). Both its oral bioavailability and enhanced Ezh1 potency can greatly complement the Ezh2-selective GSK126 in in vitro and in vivo studies.
生化/生理作用
Cell permeable: yes
Primary Target
Ezh2
Ezh2
Reversible: yes
Secondary Target
Ezh1
Ezh1
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Konze, K.D., et al. 2013. ACS Chem. Biol.8, 1324.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
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