| Bioactivity | MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, 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]. | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | MG-277 | ||||||||||||
| CAS | 2411085-89-5 | ||||||||||||
| Formula | C41H42Cl2FN5O5 | ||||||||||||
| Molar Mass | 774.71 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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MG-277
CAS: 2411085-89-5 F: C41H42Cl2FN5O5 W: 774.71
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon
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