JUN-1111

Names

[ CAS No. ]:
874351-38-9

[ Name ]:
JUN-1111

[Synonym ]:
jun-1111
unii-fm4058y01h

Biological Activity

[Description]:

JUN-1111 is an irreversible and selective Cdc25 phosphatase inhibitor with IC50 values of 0.38, 1.8, 0.66, 28, 37 µM for Cdc25A, Cdc25B, Cdc25C, VHR, PTP1B, respectively. JUN-1111 induces cell cycle arrest at G1 and G2/M phases. JUN-1111 decreases the expression of phosphoCdk1[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphatase

[Target]

IC50:0.38 µM (Cdc25A); 1.8 µM (Cdc25B); 0.66 µM (Cdc25C); 28 µM (VHR); 37 µM (PTP1B)[1]


[In Vitro]

JUN-1111 (10, 30 µM; 17 h) 在 tsFT210 细胞中诱导细胞周期停滞在 G1 和 G2/M 期[1]。 JUN-1111 (10, 30 µM; 1 h) 以剂量依赖性方式降低 tsFT210 细胞中 phosphoCdk1 的表达[1]。 JUN-1111 (0-20 µM) 在哺乳动物细胞中诱导活性氧的形成[2]。 Cell Cycle Analysis[1] Cell Line: tsFT210 cells Concentration: 10, 30 µM Incubation Time: 17 h Result: Induced cell cycle arrest at G1 and G2/M phases. Western Blot Analysis[1] Cell Line: tsFT210 cells Concentration: 10, 30 µM Incubation Time: 1 h Result: Decreased the expression of phosphoCdk1 in a dose-dependent manner.

[References]

[1]. Brisson M, et al. Redox regulation of Cdc25B by cell-active quinolinediones. Mol Pharmacol. 2005 Dec;68(6):1810-20.  

[2]. Vogt A, et al. A cell-active inhibitor of mitogen-activated protein kinase phosphatases restores paclitaxel-induced apoptosis in dexamethasone-protected cancer cells. Mol Cancer Ther. 2008 Feb;7(2):330-40.  

Chemical & Physical Properties

[ Molecular Formula ]:
C15H17N3O3

[ Molecular Weight ]:
287.31400

[ Exact Mass ]:
287.12700

[ PSA ]:
71.53000

[ LogP ]:
0.59510


Related Compounds