MG-277

MG-277是一种分子胶降解剂，可有效诱导翻译终止因子GSPT1的降解，DC50为1.3nM。MG-277以非p53的方式高度有效地抑制肿瘤细胞的生长，对RS4;11细胞和p53突变体RS4;11/IRMI-2细胞的IC50分别为3.5nM和3.4nM。MG-277具有有效的抗癌活性。

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库存: 现货

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5mg

￥19762.00

15810.00

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10mg

￥32062.00

25650.00

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25mg

￥53437.00

42750.00

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已选 0 种 0 瓶

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Background

MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity[1].

MG-277 (0.03-10 nM; 24 hours; RS4;11 cells) treatment inhibits cell growth and degrades GSPT1[1].MG277 has a significantly decreased potency in reducing the level of MDM2 protein in cells and fails to activate wild-type p53. MG-277 is highly potent and effective in inhibition of cell growth in cancer cell lines with wild-type p53, mutated p53, or deleted p53, indicating a p53-independent mechanism. MG-277 induces rapid GSPT1 degradation in cancer cells in a p53- and MDM2-independent manner but in a manner dependent upon cereblon, CUL4 E3 ubiquitin ligase, and proteasomes[1]. Western Blot Analysis[1] Cell Line: RS4;11 cells

[1]. Yang J, et al. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders. J Med Chem. 2019 Oct 21.