KEA1-97 是一种选择性Thioredoxin-caspase 3相互作用干扰剂 (IC50=10 μM)。KEA1-97 在不影响 thioredoxin 活性的情况下, 破坏 thioredoxin 与 caspase 3 的相互作用, 激活 caspases, 诱导细胞 apoptosis。
货号:ajcx34886
CAS:2138882-71-8
分子式:C15H9Cl2FN4
分子量：335.16
溶解度:DMSO : 100 mg/mL (298.36 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

KEA1-97 is a selective Thioredoxin-caspase 3 interaction disruptor (IC50=10 μM). KEA1-97 disrupts the interaction of thioredoxin with caspase 3, activates caspases, and induces apoptosis without affecting thioredoxin activity[1].

KEA1-97 (100 μM; 231MFP cells) impaires thioredoxin pulldown of caspase 3[1].KEA1-97 (10 μM; 48 hours; 231MFP cells) impaires 231MFP serum-free cell proliferation[1].KEA1-97 (10 μM; 0~12 hours; 231MFP cells) activates caspase 3/7 and induces apoptotic cell death[1].KEA1-97 (231MFP cells) resistants to survival and proliferation impairments[1].

KEA1-97 (5 mg/kg; i.p.; 50 days) attenuates tumor xenograft growth[1].

[1]. Anderson KE, et al. Chemoproteomics-Enabled Covalent Ligand Screening Reveals a Thioredoxin-Caspase 3 Interaction Disruptor That Impairs Breast Cancer Pathogenicity. ACS Chem Biol. 2017;12(10):2522-2528.