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UNC0646 {[allProObj[0].p_purity_real_show]}

货号:A880677 Ambeed 开学季,买赠积分,赢豪礼

UNC0646 is a potent and selective G9a inhibitor with IC50 of 6 nM.

UNC0646 化学结构 CAS号:1320288-17-2
UNC0646 化学结构
CAS号:1320288-17-2
UNC0646 3D分子结构
CAS号:1320288-17-2
UNC0646 化学结构 CAS号:1320288-17-2
UNC0646 3D分子结构 CAS号:1320288-17-2
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UNC0646 纯度/质量文件 产品仅供科研

货号:A880677 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 {[allProObj[0].p_purity_real_show]}
UNC1999 +++

EZH2, IC50: 2 nM

EZH1, IC50: 45 nM

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EPZ005687 ++

EZH2, Ki: 24 nM

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EPZ015666 +++

PRMT5, Ki: 5 nM

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3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

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EPZ6438 +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

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GSK126 ++

EZH2, IC50: 9.9 nM

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MI-3 +

Menin-MLL, IC50: 648 nM

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MM-102 ++

MLL1, IC50: 0.4 μM

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EI1 ++

Ezh2 (wild-type), IC50: 15 nM

EZH2 (Y641F), IC50: 13 nM

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SGC0946 ++++

DOT1L, IC50: 0.3 nM

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PFI-2 HCl ++++

SETD7, IC50: 2 nM

SETD7, Ki: 0.33 nM

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Pinometostat ++++

DOT1L, Ki: 80 pM

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EPZ004777 +++

DOT1L, IC50: 0.4 nM

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Entacapone ++

COMT, IC50: 151 nM

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UNC0379 +

SETD8, IC50: 7.9 μM

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Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

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GSK343 +++

EZH2, IC50: 4 nM

EZH1, IC50: 240 nM

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BIX-01294 3HCl +

G9a, IC50: 2.7 μM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

UNC0646 生物活性

描述 The lysine methyltransferase G9a is overexpressed in many human cancers. UNC0646 is a potent G9a inhibitor with an IC50 value of 6nM in the SAHH-coupled assay. The H3K9me2 antibody cell immunofluorescence In-Cell Western (ICW) assay showed that the IC50 values of UNC0646 for reducing H3K9me2 levels in MDA-MB-231, MCF7, PC3, 22RV1, HCT116 wt, HCT116 p53−/−, and IMR90 cell lines were 26, 10, 12, 14, 68, 86, and 10nM, respectively. The toxicity (EC50) of UNC0646 in these cell lines were 3.3, 4.7, 2.8, 7.2, 8.7, 12, and 3.6μM, respectively. UNC0646 is also a potent GLP inhibitor with an IC50 value of < 15nM[2]. In an orthotopic hepatocellular carcinoma mouse model, nanodiamond-mediated delivery of UNC0646 at a dosage of 2mg/kg significantly inhibited tumor growth compared to the control groups. The ND-UNC0646 treated group also showed minimal positive Ki67 staining, no tissue morphological alterations or inflammation in tumor tissues[3].

UNC0646 参考文献

[1]Liu F, Barsyte-Lovejoy D, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50.

[2] Liu F, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines. J Med Chem. 2011 Sep 8;54(17):6139-50

[3]Gu M, Toh TB, Hooi L, Lim JJ, Zhang X, Chow EK. Nanodiamond-Mediated Delivery of a G9a Inhibitor for Hepatocellular Carcinoma Therapy. ACS Appl Mater Interfaces. 2019 Dec 11;11(49):45427-45441

UNC0646 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.04mL

1.61mL

0.80mL

16.08mL

3.22mL

1.61mL

UNC0646 技术信息

CAS号1320288-17-2
分子式C36H59N7O2
分子量 621.899
别名
运输蓝冰
存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 35 mg/mL(56.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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