1. PROTAC
    Apoptosis
  2. PROTAC
    Apoptosis
  3. MG-277

MG-277 

Cat. No.: HY-130122
Handling Instructions

MG-277 is a molecular glue compound transformed from PROTAC degradation agent. MG-277 induces moderate MDM2 degradation. 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. MG-277 effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 has potent anticancer activity.

For research use only. We do not sell to patients.

MG-277 Chemical Structure

MG-277 Chemical Structure

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Description

MG-277 is a molecular glue compound transformed from PROTAC degradation agent. MG-277 induces moderate MDM2 degradation. 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. MG-277 effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 has potent anticancer activity[1].

IC50 & Target[1]

MDM2

 

In Vitro

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
Concentration: 0.03 nM, 0.1 nM, 0. 3 nM, 1 nM, 3 nM, 10 nM
Incubation Time: 24 hours
Result: Degraded GSPT1.
Molecular Weight

774.71

Formula

C₄₁H₄₂Cl₂FN₅O₅

SMILES

ClC1=CC=C2C(NC([[email protected]@]23C4(N[[email protected]]([[email protected]@H]3C5=CC=CC(Cl)=C5F)C(NCCCCCC6=C(C7=CC=C6)CN(C7=O)C8C(NC(CC8)=O)=O)=O)CCCCC4)=O)=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MG-277MG277MG 277PROTACApoptosisProteolysis-targeting chimeraCancercellgrowthMDM2GSPT1degradationmolecularglueInhibitorinhibitorinhibit

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MG-277
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HY-130122
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