说明： CA3 (CIL56) 对YAP1/Tead转录活性具有有效的抑制作用，主要靶向高表达YAP1、具有癌症干细胞属性的、难治疗的食管腺癌细胞。CA3(CIL56)可诱导铁死亡和铁依赖的活性氧自由基。 Information 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) . Targets YAP/TEAD interaction 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. In vivo CA3 exerts strong antitumor activity in xenograft model with no apparent toxicity. Cell Research(from reference) Cell lines：SKGT-4 and JHESO cells Concentrations：0.5 and 1 μmol/L Incubation Time：48 hours
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CA3 (CIL56)
CAS number：300802-28-2 molecular formula：C23H27N3O5S2
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| Chinese alias | 1,1'-[[9-(羟基亚氨基)-9H-芴-2,7-二基]双(磺酰基)]双哌啶 | ||
| English alias | 2,7-bis(1-Piperidinylsulfonyl)-9H-fluoren-9-one oxime | CIL56 | 1,1′-[[9-(Hydroxyimino)-9H-fluorene-2,7-diyl]bis(sulfonyl)]bis-piperidine | ||
| CAS number | 300802-28-2 | molecular formula | C23H27N3O5S2 |
| molecular weight | 489.61 g/mol | Exact mass | ≥97% |
| PSA | 124.000 Ų | logp | 3.058 |
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