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 Experiment | |
---|---|
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 |
Animal Experiment | |
---|---|
Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 489.61 |
Formula | C23H27N3O5S2 |
CAS Number | 300802-28-2 |
Solubility (25°C) | 35 mg/mL in DMSO (May need ultrasonic) |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
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.
[2] Lu L, et al. Neuron. Topography of Place Maps along the CA3-to-CA2 Axis of the Hippocampus.
Related Ferroptosis Products |
---|
PRDX3(103-112) SO3 modified, human
PRDX3(103-112) SO3 modified, human is a marker of ferroptosis, and can be used for liver diseases study. |
PRDX3(103-112), human
PRDX3(103-112), human is a marker for ferroptosis. |
GPX4-IN-3
GPX4-IN-3 is a potent glutathione peroxidase 4 (GPX4) inhibitor that selectively induces ferroptosis.1 μM of GPX4-IN-3 inhibited 71.7% of GPX4 activity. |
YL-939
YL-939 is a potent ferroptosis inhibitor that inhibits iron death by targeting the PHB2/ferritin/iron axis. |
MMRi62
MMRi62 is a ferroptosis inducer targeting MDM2-MDM4 (negative regulator of the oncogene p53), which induces ferroptosis accompanied by an increase in reactive oxygen species (ROS) and lysosomal degradation of ferritin heavy chain (FTH1).MMRi62 displays p53-independent apoptosis activity and induces autophagy in pancreatic ductal adenocarcinoma (PDAC) cells. MMRi62 shows p53-independent pro-apoptosis activity and induces autophagy in pancreatic ductal adenocarcinoma (PDAC) cells.) In addition, MMRi62 caused proteasomal degradation of mutant p53 and was active in vivo in an in situ xenograft PDAC mouse model characterized by high-frequency mutations in KRAS and TP53. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.