Bioactivity | 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]. | ||||||||||||
Target | IC50:0.38 µM (Cdc25A); 1.8 µM (Cdc25B); 0.66 µM (Cdc25C); 28 µM (VHR); 37 µM (PTP1B) | ||||||||||||
Invitro | 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: | ||||||||||||
Name | JUN-1111 | ||||||||||||
CAS | 874351-38-9 | ||||||||||||
Formula | C15H17N3O3 | ||||||||||||
Molar Mass | 287.31 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |