2131-61-5Relevant articles and documents
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Marquordt
, p. 1716 (1966)
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Anionic fluorescent probe, preparation method and application thereof
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Paragraph 0032; 0043-0044, (2021/05/01)
The invention discloses an anionic fluorescent probe, and a preparation method and an application thereof. The anionic fluorescent probe is prepared by mixing 1-(4-amino) phenyl-1, 2, 2-triphenylethylene with a phenyl isothiocyanate derivative and carrying out a condensation reaction. The fluorescent probe has selectivity on anions and can be used for quantitatively analyzing the recognized anions.
Discovery of novel USP8 inhibitors via Ubiquitin-Rho-110 fluorometric assay based high throughput screening
Bian, Jinlei,Chen, Kaixian,Ding, Hong,Han, Jie,Jiang, Hualiang,Li, Zhiyu,Luo, Cheng,Ma, Zengyi,Tian, Yucheng,Wang, Jubo,Xu, Xi,Yu, Liang,Zhang, Qilin,Zhang, Yichao,Zhao, Yao
, (2020/06/01)
USP8, one member of deubiquitinating enzymes (DUBs) families, maintains the ubiquitination level of EGFR and regulates the downstream signaling pathways. The deregulation of USP8 has been implicated in many human diseases, especially in cancer. Therefore, USP8 has been identified as a promising target for drug design. Herein, via high throughput screening based on Ubiquitin-rhodamine-110 (Ubiquitin-Rho-110) fluorometric activity assay, we discovered a novel inhibitor DC-U43. By structure optimization, DC-U43-10 reached a half-maximal inhibitory concentration (IC50) value of 2.6 ± 1.1 μM and exhibited 10-fold selectivity against USP7. The binding between DC-U43-10 and USP8 was validated by surface plasmon resonance (SPR) assay with a KD value of 10.5 ± 3.7 μM. It also inhibited the colony formation of H1975 cells. Hence, DC-U43-10 represents a kind of USP8 inhibitors with novel scaffold and has broad prospects for being a probe for USP8-related academic and clinical research.