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Chemical Structure| 2505001-62-5 Chemical Structure| 2505001-62-5

Structure of SR18662
CAS No.: 2505001-62-5

Chemical Structure| 2505001-62-5

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SR18662 is a potent inhibitor of Krüppel-like factor five (KLF5) with an IC50 of 4.4 nM and an analogue of ML264 (HY-19994) with improved inhibitory potency against colorectal cancer cells. SR18662 can be used for the study of colorectal cancer.

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Product Citations

Product Citations

Dharmendra Bhargava ; David Rusakow ; Wilson Zhang ; Silina Awad ; Jonathan P. Katz ;

Abstract: The transcriptional regulator Krüppel -like factor 5 (KLF5 ) is highly expressed in squamous epithelial cells of the esophagus. Increased KLF5 activity induce s tumorigenesis and promotes metastasis in several cancers, although this function appears to be context -dependent. Here, we demonstrate that acute KLF5 inhibition, both genetically and with the potent KLF5 inhibitor ML264, causes non -transformed human primary esophageal squamous epithelial cells to enter the epithelial to mesenchymal transition (EMT). Moreover, chronic KLF5 inhibition with ML264 leads to the development of cells with a mesenchymal phenotype characterized by the expression of mesenchymal markers and functionally by reduced cell growth and increased migration and cellular invasion. This EMT resulting from chronic KLF5 inhibition is not driven by β -Catenin or TGF -β signaling. Pharmacologically, ML264 inhibits KLF5 by promoting proteasomal -mediated degradation. Taken together, we demonstrate that reduced KLF5 activity reprogram s epithelial cells towards a mesenchymal phenotype and enhance s their migratory and invasive potential. These findings have potential implications not only for esophageal cancer s but also for normal processes such as esophageal tissue repair following injury.

Keywords: KLF5 ; EMT ; epithelial ; migration ; invasion

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Product Details of SR18662

CAS No. :2505001-62-5
Formula : C16H19Cl2N3O4S
M.W : 420.31
SMILES Code : O=C(NCC(N1CCN(S(=O)(C)=O)CC1)=O)/C=C/C2=CC=C(Cl)C(Cl)=C2
MDL No. :MFCD32693929
InChI Key :WUJBXFXHDUVSFM-HWKANZROSA-N
Pubchem ID :146674222

Safety of SR18662

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P264-P270-P271-P280-P301+P312-P302+P352-P304+P340-P305+P351+P338-P330-P332+P313-P337+P313-P362-P403+P233-P405-P501

Related Pathways of SR18662

MAPK

Isoform Comparison

Biological Activity

Description
SR18662, an analog of ML264, exhibits enhanced inhibitory potency against colorectal cancer cells by effectively targeting Krüppel-like factor five (KLF5) with an IC50 value of 4.4 nM. It serves as a valuable tool for colorectal cancer research[1].

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.90mL

2.38mL

1.19mL

23.79mL

4.76mL

2.38mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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