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ML264

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Chemical Structure| 1550008-55-3 同义名 : CID-51003603
CAS号 : 1550008-55-3
货号 : A183374
分子式 : C17H21ClN2O4S
纯度 : 99%+
分子量 : 384.878
MDL号 : MFCD30187519
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(272.81 mM)，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：
生物活性
描述 The Kruppel-like factors (KLFs) are a family of transcription factors that contain zinc finger, which could regulate various cellular processes including proliferation, differentiation, development and apoptosis [1] . ML264 is an inhibitor of one of the KLF member, the KLF5, with IC50 value of 29 nM [2] .
The DLD-1 and HCT116 cells were treated with 10 μmol/L of ML264. For the cell proliferation experiment, a significant decrease in proliferation of both cells lines was observed within 24 hours of incubation. Western blot analysis showed that the protein levels of ERK and KLF5 were decreased in both DLD-1 and HCT116 cells after 72 hours of ML264 treatment. Both cell lines showed a reduction in the level of the transcription factor early growth response 1 (EGR1) which is a direct activator of KLF5 expression. [3] . Similar results could be seen on HCT116 and MDA-MB-468 cell lines [4] .
In DLD-1 tumor xenografts nude mice model, the ML264 was injected intraperitoneally for 10 days with 10 mg/kg or 25 mg/kg twice per day, and the tumor growth was significantly inhibited. The expression of the KLF5 and EGR1 in the xenografts from mice was significantly reduced after the ML264 treatment measured by IHC and western blot analysis [3] .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

12.99mL

2.60mL

1.30mL

25.98mL

5.20mL

2.60mL
参考文献

[1]McConnell BB, Ghaleb AM, et al. The diverse functions of Krüppel-like factors 4 and 5 in epithelial biology and pathobiology. Bioessays. 2007;29(6):549-57.

[2]Bialkowska A, Crisp M, et al. ML264: An Antitumor Agent that Potently and Selectively Inhibits Kruppel-like Factor Five (KLF5) Expression: A Probe for Studying Colon Cancer Development and Progression. 2011 Oct 31 [updated 2013 Mar 7] . Probe Reports from the NIH Molecular Libraries Program [Internet] . Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK143546/

[3]Ruiz de Sabando A, Wang C, et al. ML264, A Novel Small-Molecule Compound That Potently Inhibits Growth of Colorectal Cancer. Mol Cancer Ther. 2016 Jan;15(1):72-83.

[4]Chen Z, Wu Q, Ding Y, et al. YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway. Theranostics. 2017;7(8):2339-2349.