Home Hippo YAP inhibitor - ROS activator - Ferroptosis activator - TEAD inhibitor CA3 (CIL56)

CA3 (CIL56)

Catalog No.S8661

For research use only.

CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).

CA3 (CIL56) Chemical Structure

CAS No. 300802-28-2

Selleck's CA3 (CIL56) has been cited by 11 Publications

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Biological Activity

Description CA3 (CIL56) has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties. CA3(CIL56) induces ferroptosis and iron-dependent reactive oxygen species (ROS).
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 NIDSWotHfW6ldHnvckBie3OjeR?= NHjPfolKdmirYnn0bY9vKG:oIGfueE9j\XSjLXPheIVvcW5idILhcpNkemmydHnvcoFtKGGldHn2bZR6KGmwIHj1cYFvKEiWLUK5JINmdGy|IHHzd4V{e2WmIHHzJIRmeGyndHnvckBw\iCkZYThMYNifGWwaX6gcIV3\WxiYomgWGNHKGy3Y3nm[ZJie2VicILvcY91\XJicnXwc5J1\XJiYYPzZZnwxIxiSVO1NF0xNjl7IN88US=> M2Dh[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4MUiyNlM5Lz5{NkG4NlI{QDxxYU6=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot YAP1 / SOX9 29167315
Immunofluorescence YAP1 / SOX9 29167315
Growth inhibition assay Cell viability 29167315
In vivo CA3 exerts strong antitumor activity in xenograft model with no apparent toxicity[1].

Protocol (from reference)

Cell Research:

[1]
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(CC1)S(=O)(=O)C2=CC3=C(C=C2)C4=C(C3=NO)C=C(C=C4)S(=O)(=O)N5CCCCC5

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04643327 Recruiting Drug: Levetiracetam|Drug: Placebo Parkinson Disease|Mild Cognitive Impairment|Memory Impairment The University of Queensland|Queensland University of Technology|Johns Hopkins University|Cleveland Clinic Lou Ruvo Center for Brain Health|Royal Brisbane and Women''s Hospital February 9 2021 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

Tech Support

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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