Skp2 Inhibitor C1 (Synonyms: SKPin C1) |
Catalog No.GC37648 |
Skp2 Inhibitor C1 (SKPin C1) es un inhibidor de molécula pequeÑa especÍfico de la degradaciÓn de p27 mediada por Skp2, inhibiÓ selectivamente la degradaciÓn de p27 mediada por Skp2 al reducir la uniÓn de p27 a través de contactos clave de compuesto-receptor.
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Cas No.: 432001-69-9
Sample solution is provided at 25 µL, 10mM.
Skp2 Inhibitor C1(SKPin C1) is a specific small molecule inhibitor of Skp2-mediated p27 degradation, selectively inhibited Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.IC50 value: Target: Skp2 inhibitor; p27 regulatorin vitro: T47D cells treated with C1 (5 μM for 16 hours) displayedan increase in G1 phase (p < 0.0001) and a decrease in S phase (p < 0.0001), correlating with p27 protein induction. In contrast, MCF-7 cells responded to C1 with a significant reduction in G1 phase (35%, p < 0.0001) and an increase in G2-M phase (43%, p < 0.0001). This G1 reduction and G2/M arrest is dose dependent on C1 (Figure 5C right; p < 0.001 and p < 0.01, respectively) and correlates with increased p27 protein levels (Figure 5E left, S4A top right) [1].
[1]. Wu L, et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. Chem Biol. 2012 Dec 21;19(12):1515-24. [2]. Pavlides SC, et al. Inhibitors of SCF-Skp2/Cks1 E3 ligase block estrogen-induced growth stimulation and degradation of nuclear p27kip1: therapeutic potential for endometrial cancer. Endocrinology. 2013 Nov;154(11):4030-45.
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