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Purity: ≥98%
CA3 (also known as CIL56) is a novel and potent inhibitor of YAP1/Tead transcriptional activity. In vitro and in vivo studies have shown that CA3 has a remarkable inhibitory effect on the growth of esophageal adenocarcinoma cells, particularly those that express high levels of the YAP1 gene. Normally, radiation-resistant cells develop strong cancer stem cell (CSC) properties and an aggressive phenotype, but CA3 can successfully suppress these phenotypes by preventing proliferation, inducing apoptosis, reducing the formation of tumor spheres, and decreasing the percentage of ALDH1+ cells.
| Targets |
YAP/TEAD interaction
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| ln Vitro |
In vitro, CA3 significantly reduces the growth of esophageal adenocarcinoma cells. Inducing apoptosis, decreasing tumor sphere formation, and reducing the number of ALDH1+ cells are all possible effects of CA3. After cotransfection of each transcriptional factor's individual promoter luciferases in 293T cells, CA3 specifically inhibits Tead/YAP1 transcriptional activity but has no effect on Super-TOP/Wnt, CBF1/Notch, or AP-1. The CSC properties that are enriched in radiation-resistant esophageal adenocarcinoma cells are preferentially inhibited by CA3[1].
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| ln Vivo |
In a xenograft model, CA3 exhibits potent antitumor activity with no discernible toxicity[1].
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| Enzyme Assay |
The SOX9 luciferase reporter was described previously. The 5 × -UAS-luciferase reporter and Gal4-TEAD4 constructs, also described previously, were obtained from Dr. Johnson of MD Anderson Cancer Center. Transient cotransfection esophageal adenocarcinoma cells with the SOX9 luciferase reporter and a Renilla vector or 5 × -UAS-luciferase reporter and Gal4-TEAD4 with a CMV-β-gal construct was performed as described previously.
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| Cell Assay |
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 exposed for 48 hours to 0.1% DMSO (control) or CA3 at various doses as recommended. The cells are then collected, fixed with methanol, washed, treated with RNase A, stained with propidium iodide for DNA, and subjected to flow cytometry analysis of DNA histograms and cell-cycle phase distributions.
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| References |
| Molecular Formula |
C23H27N3O5S2
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| Molecular Weight |
489.61
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| Exact Mass |
489.14
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| Elemental Analysis |
C, 56.42; H, 5.56; N, 8.58; O, 16.34; S, 13.10
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| CAS # |
300802-28-2
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
C1CCN(CC1)S(=O)(=O)C2=CC3=C(C=C2)C4=C(C3=NO)C=C(C=C4)S(=O)(=O)N5CCCCC5
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| InChi Key |
XYZXEEIUKQGUHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H27N3O5S2/c27-24-23-21-15-17(32(28,29)25-11-3-1-4-12-25)7-9-19(21)20-10-8-18(16-22(20)23)33(30,31)26-13-5-2-6-14-26/h7-10,15-16,27H,1-6,11-14H2
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| Chemical Name |
N-[2,7-bis(piperidin-1-ylsulfonyl)fluoren-9-ylidene]hydroxylamine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.11 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O: 0.5mg/ml |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0424 mL | 10.2122 mL | 20.4244 mL | |
| 5 mM | 0.4085 mL | 2.0424 mL | 4.0849 mL | |
| 10 mM | 0.2042 mL | 1.0212 mL | 2.0424 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04643327 | Recruiting | Drug: Levetiracetam Drug: Placebo |
Parkinson Disease Memory Impairment |
The University of Queensland | February 9, 2021 | Phase 2 |
| NCT03896659 | Recruiting | Drug: Hydrocortisone Oral Drug: Placebo Oral Tablet |
Depression Hydrocortisone |
University of Texas Southwestern Medical Center |
October 1, 2019 | Phase 4 |
| NCT04951700 | Recruiting | Other: Other | Aging Schizophrenia |
University of Texas Southwestern Medical Center |
July 1, 2021 | |
| NCT01522560 | Completed | Other: Feedback group Other: Control group |
Pediatric Anesthesia Department |
The Cleveland Clinic | July 2011 | Not Applicable |
Identification of novel YAP1 inhibitor CA3 and determination of its effects on YAP1 high esophageal adenocarcinoma cells.Mol Cancer Ther.2018 Feb;17(2):443-454. |
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CA3 potently inhibits esophageal adenocarcinoma cell growth and induces tumor cell death.Mol Cancer Ther.2018 Feb;17(2):443-454. |
CA3 inhibits YAP1 expression and transcriptional activity in esophageal adenocarcinoma cell lines, especially those with high YAP1.Mol Cancer Ther.2018 Feb;17(2):443-454. |
CA3 preferentially inhibits CSC properties enriched in radiation-resistant esophageal adenocarcinoma cells.Mol Cancer Ther.2018 Feb;17(2):443-454. |
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CA3 suppresses ALDH1+cell tumor sphere and exerts strong antitumor effects in inducible high YAP xenograft model.Mol Cancer Ther.2018 Feb;17(2):443-454. |
CA3 synergizes with 5-FU in inhibiting growth of esophageal adenocarcinoma cellsin vitroandin vivo.Mol Cancer Ther.2018 Feb;17(2):443-454. |
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