| CAS NO: | 432001-69-9 |
| Cas No. | 432001-69-9 |
| 别名 | SKPin C1 |
| Canonical SMILES | S=C(S/1)N(CC2=CN=CC=C2)C(C1=C\C(C=C(Br)C=C3)=C3OCC(O)=O)=O |
| 分子式 | C18H13BrN2O4S2 |
| 分子量 | 465.34 |
| 溶解度 | DMSO: 25 mg/mL (53.72 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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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