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.
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Nutlin-3b
CAS number:675576-97-3 molecular formula:C30H30Cl2N4O4
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compound introduction
Specs
| Chinese alias | 纽特林-3b | ||
| English alias | (+/-)-4-[4,5-Bis(4-chlorophenyl)-2-(2-isopropoxy-4-methoxy-phenyl)-4,5-dihydro-imidazole-1-carbonyl]-piperazin-2-one | CHEBI:46742 | rel-4-{[(4R,5S)-4,5-bis(4-chlorophenyl)-2-{2-[(propan-2-yl)oxy]-4-methoxyphenyl}-4,5-dihydro-1H-imidazol-1-yl]carbonyl}pip | ||
| CAS number | 675576-97-3 | molecular formula | C30H30Cl2N4O4 |
| molecular weight | 581.49 g/mol | Exact mass | ≥98% |
| PSA | 83.500 Ų | logp | 5.200 |
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