CIL56 (CA3) is a potent and selective ferroptosis inducer, it has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
In vitro: CIL56 (CA3) strongly inhibits esophageal adenocarcinoma cell growth in vitro. CIL56 (CA3) can effectively suppress tumor cell proliferation, induce apoptosis, reduce tumor sphere formation, and the population of ALDH1+ cells. CIL56 (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. CIL56 (CA3) preferentially inhibits CSC properties enriched in radiation-resistant esophageal adenocarcinoma cells.
In vivo: CIL56 (CA3) exerts strong antitumor activity in xenograft model with no apparent toxicity.
|Cell lines||SKGT-4 and JHESO cells|
|Preparation 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.|
|Concentrations||0.5 and 1 μmol/L|
|Incubation time||48 hours|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||35 mg/mL in DMSO (May need ultrasonic)|
Aging-Related Hyperexcitability in CA3 Pyramidal Neurons Is Mediated by Enhanced A-Type K+ Channel Function and Expression.
Simkin D, et al. J Neurosci. 2015 Sep 23;35(38):13206-18. PMID: 26400949.
Topography of Place Maps along the CA3-to-CA2 Axis of the Hippocampus.
Lu L, et al. Neuron. 2015 Sep 2;87(5):1078-92. PMID: 26298277.
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