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GSK2879552 2HCl

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Chemical Structure| 1902123-72-1 同义名 : GSK2879552 dihydrochloride
CAS号 : 1902123-72-1
货号 : A567729
分子式 : C23H30Cl2N2O2
纯度 : 99%+
分子量 : 437.402
MDL号 : MFCD30481342
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(68.59 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

H2O: 100 mg/mL(228.62 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • KDM1

    LSD1, Ki:1.7 μM
描述 The lysine-specific demethylase (LSD1) is a Flavin-dependent amine oxidase that selectively removes one or two methyl groups from histone H3 at the Lys4 position. Along with histone deacetylases 1 and 2, LSD1 is involved in epigenetically silencing gene expression, and has been implicated as a potential therapeutic target in cancer and other diseases[2]. GSK2879552 2HCl is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity[3]. A proliferation screen of cell lines representing a number of tumor types indicated that small cell lung carcinoma (SCLC) was sensitive to LSD1 inhibition. The SCLC lines that undergo growth inhibition in response to GSK2879552 exhibit DNA hypomethylation of a signature set of probes suggesting this may be used as a predictive biomarker of activity[4]. The mice were treated with either vehicle or GSK2879552 (5 mg/kg) for 4 weeks with the sizes of the tumors monitored every other day. The tumors in mice treated with GSK2879552 are not only much smaller but also weigh much lesser. The effect of GSK2879552 in the patient-derived xenograft (PDX) model used metastatic BCa tissues and found that GSK2879552 is capable of inhibiting the growth of PDX significantly. Furthermore, the results of IHC showed the levels of Ki67 and Bcl-2 in xenografts derived from either cancer cells or PDX were also inhibited by GSK2879552[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.43mL

2.29mL

1.14mL

22.86mL

4.57mL

2.29mL
参考文献

[1]Mohammad HP, Smitheman KN, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69.

[2]D Hayward, P A Cole. LSD1 Histone Demethylase Assays and Inhibition. Methods Enzymol.2016. 573, 261-78.

[3]Adam Albanese,et al. The Role of Hypoxia-Inducible Factor Post-Translational Modifications in Regulating Its Localisation, Stability, and Activity. Int J Mol Sci. 2020. 22(1), 268.

[4]Helai P Mohammad, Ryan G Kruger. Antitumor activity of LSD1 inhibitors in lung cancer. Mol Cell Oncol.2016. 3(2), e1117700.

[5]Qiubo Xie, Tang Tang,et al. LSD1 Promotes Bladder Cancer Progression by Upregulating LEF1 and Enhancing EMT. Front Oncol. 2020. 10, 1234.