CA3 (CIL56)

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

CA3 (CIL56) Chemical Structure

CAS No. 300802-28-2

Purity & Quality Control

CA3 (CIL56) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT-29 cells Function assay Inhibition of Wnt/beta-catenin transcriptional activity in human HT-29 cells assessed as depletion of beta-catenin level by TCF luciferase promoter reporter assay, IC50=0.99 μM 26182238
Click to View More Cell Line Experimental Data

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
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 Research 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.

Experimental Result Images Methods Biomarkers Images PMID
Western blot YAP1 / SOX9 29167315
Immunofluorescence YAP1 / SOX9 29167315
Growth inhibition assay Cell viability 29167315
In Vivo
In vivo

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

Animal Research Animal Models A JHESO xenograft model of esophageal adenocarcinoma
Dosages 1 mg/kg/mouse
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04643327 Recruiting
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

Chemical Information & Solubility

Molecular Weight 489.61 Formula

C23H27N3O5S2

CAS No. 300802-28-2 SDF Download CA3 (CIL56) SDF
Smiles C1CCN(CC1)S(=O)(=O)C2=CC3=C(C=C2)C4=C(C3=NO)C=C(C=C4)S(=O)(=O)N5CCCCC5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 97 mg/mL ( (198.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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. )

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

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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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