ML264

製品コードS8196 バッチS819601

印刷

化学情報

 Chemical Structure Synonyms CID-51003603 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C17H21ClN2O4S

分子量 384.88 CAS No. 1550008-55-3
Solubility (25°C)* 体外 DMSO 76 mg/mL (197.46 mM)
Water Insoluble
Ethanol Insoluble
体内 (毎回新しく調製した物を用意してください)
Clear solution
5%DMSO Corn oil
3.8mg/ml Taking the 1 mL working solution as an example, add 50 μL of 76 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 ML264 (CID-51003603), a selectively inhibitor of kruppel-like factor 5 (KLF5),potently Inhibits Growth of Colorectal Cancer.
in vitro ML264 potently halts DLD-1 viability (IC50 = 29 nM) with high maximal effect (>90%). DLD-1 cells are human colorectal adenocarcinoma cells. ML264 has significant effects at submicromolar doses on other cell types as well, including HCT116 (human colorectal carcinoma), HT29 (human colorectal adenocarcinoma), and SW620 (human colorectal adenocarcinoma). The IEC-6 anti-target (a nontransformed rat intestinal epithelial cell line) is largely unaffected, with inhibition below 50% at the highest dose[1].This compound potently inhibits proliferation of CRC cells in vitro through modifications of the cell cycle profile[2].
in vivo In an established xenograft mouse model of colon cancer, ML264 efficiently inhibits growth of the tumor within five days of treatment. this effect is caused by a significant reduction in proliferation and that ML264 potently inhibits the expression of KLF5 and EGR1, a transcriptional activator of KLF5[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 DLD-1 and HCT116 colorectal cancer cell lines
濃度 10μM
反応時間 24, 48, 72h
実験の流れ

For cell proliferation experiments, DLD-1 and HCT116 cells are treated with 10μM ML264 or with vehicle (DMSO). Live cells are collected at 24, 48 and 72 hours post treatment and their numbers are determined by counting using a Coulter counter; In MTS assay, DLD-1 and HCT116 cells are treated with 10μM ML264 or with vehicle (DMSO). After 24, 48, and 72 hours of incubations, 20 μL of MTS solution  is added to each well and an analysis is performed according to the manufacturer's protocol.

動物実験 動物モデル Nude mice with DLD-1 cells injection to achieve a tumor
投薬量 10 or 25 mg/kg
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Krüppel-like factor 5 promotes the progression of oral squamous cell carcinoma via the baculoviral IAP repeat containing 5 gene [ Ann Transl Med, 2022, 10(18):969] PubMed: 36267746
Oxidative Stress-Induced Hypermethylation of KLF5 Promoter Mediated by DNMT3B Impairs Osteogenesis by Diminishing the Interaction with β-Catenin [ Antioxid Redox Signal, 2021, 10.1089/ars.2020.8200] PubMed: 33588625
Nucleotide variation in histone H2BL drives crossalk of histone modification and promotes tumour cell proliferation by upregulating c-Myc [ Life Sci, 2021, 271:119127] PubMed: 33515561
Long intergenic noncoding RNA 00908 promotes proliferation and inhibits apoptosis of colorectal cancer cells by regulating KLF5 expression [ J Cell Physiol, 2021, 236(2):889-899] PubMed: 33020901
Long intergenic noncoding RNA 00908 promotes proliferation and inhibits apoptosis of colorectal cancer cells by regulating KLF5 expression [ J Cell Physiol, 2021, 236(2):889-899] PubMed: 33020901
Demethylation of G-Protein-Coupled Receptor 151 Promoter Facilitates the Binding of Krüppel-Like Factor 5 and Enhances Neuropathic Pain after Nerve Injury in Mice [ J Neurosci, 2018, 38(49):10535-10551] PubMed: 30373770

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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