MG-277

For research use only. Not for therapeutic Use.

  • CAT Number: I017738
  • CAS Number: 2411085-89-5
  • Molecular Formula: C₄₁H₄₂Cl₂FN₅O₅
  • Molecular Weight: 774.71
  • Purity: ≥95%
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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].<br>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].


Catalog Number I017738
CAS Number 2411085-89-5
Molecular Formula C₄₁H₄₂Cl₂FN₅O₅
Purity ≥95%
Target Apoptosis
Reference

[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.

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