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MG-277 | MG-277 : Molecular Glue of GSPT1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
GSPT1
  • IC50:67.5 nM
  • DC50:1.3 (R), 24.6 (MO), 7.9 (MV) nM
Molecular Glues
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Unbiased proteomic analysis using the RS4;11 cells with wild-type p53 and the RS4;11/IRMI-2 cells ...

Potency
Cellular
In Vitro

GSPT1

Mode of Action: Molecular Glues

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.9b00846

Orthogonal Probes def

CC-90009

Chemical Information

Molecular Formula C41H42Cl2FN5O5
SMILEs O=C1CCC(N2Cc3c(CCCCCNC(=O)[C@@H]4NC5(CCCCC5)[C@@]5(C(=O)Nc6cc(Cl)ccc65)[C@H]4c4cccc(Cl)c4F)cccc3C2=O)C(=O)N1
InChI InChI=1S/C41H42Cl2FN5O5/c42-24-14-15-28-30(21-24)46-39(54)41(28)33(26-12-8-13-29(43)34(26)44)35(48-40(41)18-4-2-5-19-40)37(52)45-20-6-1-3-9-23-10-7-11-25-27(23)22-49(38(25)53)31-16-17-32(50)47-36(31)51/h7-8,10-15,21,31,33,35,48H,1-6,9,16-20,22H2,(H,45,52)(H,46,54)(H,47,50,51)/t31?,33-,35+,41+/m0/s1
Molecular weight 773.25 Da
AlogP 6.071100000000005
HBond acceptors 10
HBond donors 4
Atoms 96

References

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canSARChEMBLBindingDB

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Expert Reviews

by SERP
(on 7 Jul 2021 )
Cellular Use Rating
MG-277 is a well-characterized degrader that depletes GSPT1 levels in several breast cancer and leukemia cell lines. The characterization included quantitative proteomic experiments (done at 100nM concentration...
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