1320288-17-2|UNC0646|CsnPharm

CAS No.: 1320288-17-2

UNC0646 Catalog No. CSN15901

Synonyms: UNC0646

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

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6080 mL
- 8.0399 mL
- 16.0798 mL
- 5 mM
- 0.3216 mL
- 1.6080 mL
- 3.2160 mL
- 10 mM
- 0.1608 mL
- 0.8040 mL
- 1.6080 mL

技术信息

CAS号

1320288-17-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C36H59N7O2

运输

蓝冰

分子量

621.90

别名

UNC0646

溶解度

DMSO	33.0 mg/mL (53.1 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (80.4 mM)

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