CA3(CIL56)

Catalog No.S8661

CA3(CIL56) Chemical Structure

Molecular Weight(MW): 489.61

CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.

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Biological Activity

Description CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
Targets
YAP/TEAD interaction [1]
()
In vitro

CA3 strongly inhibits esophageal adenocarcinoma cell growth in vitro. CA3 can effectively suppress tumor cell proliferation, induce apoptosis, reduce tumor sphere formation, and the population of ALDH1+ cells. CA3 specially inhibits Tead/YAP1 transcriptional activity but shows no inhibitory activity on other transcriptional factors-Super-TOP/Wnt, CBF1/Notch, and AP-1 after cotransfection of their respective individual promoter luciferases in 293T cells. CA3 preferentially inhibits CSC properties enriched in radiation-resistant esophageal adenocarcinoma cells[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 cells NIfWcnpHfW6ldHnvckBie3OjeR?= NHnEfYRKdmirYnn0bY9vKG:oIGfueE9j\XSjLXPheIVvcW5idILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHj1cYFvKEiWLUK5JINmdGy|IHHzd4V{e2WmIHHzJIRmeGyndHnvckBw\iCkZYThMYNifGWwaX6gcIV3\WxiYomgWGNHKGy3Y3nm[ZJie2VicILvcY91\XJicnXwc5J1\XJiYYPzZZnwxIxiSVO1NF0xNjl7IN88US=> MUWyOlE5OjJ|OB?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
YAP1 / SOX9 ; 

PubMed: 29167315     


Cell lysate from SKGT-4 and JHESO EAC cells treated with CA3 at indicated dosage were selected for immunoblotting analysis for YAP1 and SOX9.

29167315
Immunofluorescence
YAP1 / SOX9 ; 

PubMed: 29167315     


Immunofluorescent staining of YAP1 and SOX9 in JHESO cells were observed by confocal microscopy (right). 

29167315
Growth inhibition assay
Cell viability; 

PubMed: 29167315     


Four EAC cell lines A.SKGT-4, Flo-1,JHESO and OACP EAC cell lines were treated with 0.1% DMSO (as control), CA3 (left) at dosage of 0.1, 0.5 and 1µM, the cells proliferation and viability were measured using MTS assay and calculated as percent of control. B. SKGT-4 (PINYAP120) cells with (DOX+) or without (DOX−) YAP1 induction were treated with 0.1% DMSO (as control), CA3 (left) at dosage of 0.1, 0.5 and 1µM, the cells proliferation and viability were measured using MTS assay and calculated as percent of control. For all experiments, values shown represent the mean and SD of at least triplicate assays.**P<0.01.

29167315
In vivo CA3 exerts strong antitumor activity in xenograft model with no apparent toxicity[1].

Protocol

Cell Research:

[1]
+ Expand
  • Cell lines: SKGT-4 and JHESO cells
  • Concentrations: 0.5 and 1 μmol/L
  • Incubation Time: 48 hours
  • Method:

    SKGT-4 and JHESO cells are seeded onto 6-well plates (1 × 105/well) in DMEM and cultured for 24 hours to allow for cell attachment. The cells are then treated with 0.1% DMSO (control) or CA3 at different doses as indicated for 48 hours. Next, the cells are harvested, fixed with methanol, washed, treated with RNase A, and stained for DNA with propidium iodide, and their DNA histograms and cell-cycle phase distributions are analyzed using flow cytometry.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (198.11 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 489.61
Formula

C23H27N3O5S2
CAS No. 300802-28-2
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID