产品介绍:Nutlin-3b是MDM2/p53抑制剂,IC50为13.6 μM。Nutlin-3b是nutlin-3的无活性异构体。
Nutlin-3是一种小分子MDM2抑制剂,可干扰MDM2介导的TP53降解。WT-TP53的稳定可导致细胞周期停滞、生长抑制和细胞凋亡。作为一种无活性的异构体,Nutlin-3b对增殖没有任何影响,对癌细胞中的基因表达也没有明显的作用。与3a(活性nutlin-3异构体)相比,nutlin-3b结合MDM2的亲和力比nutlin-3a低200倍,活性比nutlin-3a小150倍。Nutlin-3b通常作为阴性对照,不能诱导MDM2、p53或p21的表达,在H460细胞系中也不影响集落形成,对细胞周期无影响。
Nutlin-3b 是一种 p53/MDM2 抑制剂,IC50 为 13.6 μM。Nutlin-3b 与 MDM2 的结合活性比 Nutlin-3a 低 150 倍。;Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.
靶点:
IC50: 13.6 μM (MDM2/p53)
参考文献:
1. Vassilev LT, et al. In vivo activation of the p53 pathway by small-molecule antagonists of MDM2. Science. 2004 Feb 6;303(5659):844-8. 2. Müller CR, et al. Potential for treatment of liposarcomas with the MDM2 antagonist Nutlin-3A. Int J Cancer. 2007 Jul 1;121(1):199-205. 3. Michaelis M, et al. Reversal of P-glycoprotein-mediated multidrug resistance by the murine double minute 2 antagonist nutlin-3. Cancer Res. 2009 Jan 15;69(2):416-21. 4. Zhang F, et al. MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport. Biochem Pharmacol. 2011 Jul 1;82(1):24-34.