CA3 (CIL56)

製品コードS8661 バッチS866102

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C23H27N3O5S2

分子量 489.61 CAS No. 300802-28-2
Solubility (25°C)* 体外 DMSO 98 mg/mL (200.15 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 CA3(CIL56)は、YAP1/Tead転写活性に対して強力な阻害効果を示し、主にYAP1高発現および治療抵抗性の食道腺がん細胞を標的とします。これらの細胞はCSC特性を備えています。CA3(CIL56)は、フェロトーシスと鉄依存性活性酸素種(ROS)を誘導します。
in vitro

CA3 (CIL56) strongly inhibits esophageal adenocarcinoma cell growth in vitro. It can effectively suppress tumor cell proliferation, induce apoptosis, reduce tumor sphere formation, and the population of ALDH1+ cells. This compound 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 (CIL56) exerts strong antitumor activity in xenograft model with no apparent toxicity.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SKGT-4 and JHESO cells
濃度 0.5 and 1 μmol/L
反応時間 48 hours
実験の流れ

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 (CIL56) 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.

動物実験 動物モデル A JHESO xenograft model of esophageal adenocarcinoma
投薬量 1 mg/kg/mouse
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/29167315/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

YAP as a therapeutic target to reverse trastuzumab resistance [ Gastric Cancer, 2025, 10.1007/s10120-025-01630-w] PubMed: 40542295
Targeting Latent HIV Reservoirs: Effectiveness of Combination Therapy with HDAC and PARP Inhibitors [ Viruses, 2025, 17(3)400] PubMed: 40143326
Blocking YAP1-Liprin-β2 interaction impedes metastasis and promotes tumor suppression in head and neck squamous carcinoma [ Sci Rep, 2025, 15(1):26968] PubMed: 40707583
SHP1 and its downstream p38/SP1/PI3K/YAP/Notch-1 signaling in trophoblast cells suppressed the progression of Preeclampsia via inhibiting proliferation of SMCs [ Sci Rep, 2025, 15(1):16205] PubMed: 40346122
GPRC5A promotes lung colonization of esophageal squamous cell carcinoma [ Nat Commun, 2024, 15(1):9950] PubMed: 39550386
Hippo-signaling-controlled MHC class I antigen processing and presentation pathway potentiates antitumor immunity [ Cell Rep, 2024, 43(4):114003] PubMed: 38527062
The Hippo pathway terminal effector TAZ/WWTR1 mediates oxaliplatin sensitivity in p53 proficient colon cancer cells [ BMC Cancer, 2024, 24(1):587] PubMed: 38741073
YAP-TEAD inhibition is associated with upregulation of an androgen receptor mediated transcription program providing therapeutic escape [ FEBS Open Bio, 2024, 10.1002/2211-5463.13901] PubMed: 39300603
EDA Fibronectin Microarchitecture and YAP Translocation During Wound Closure [ bioRxiv, 2024, 2024.09.23.614581] PubMed: 39386582
Microglia replacement by ER-Hoxb8 conditionally immortalized macrophages provides insight into Aicardi-Goutières Syndrome neuropathology [ bioRxiv, 2024, 2024.09.18.613629] PubMed: 39345609

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。