BAY-277
BAY-277 is a selective METAP2 degrader and inhibitor. BAY-277 induces ubiquitination and proteasomal degradation of METAP2, triggers G1-phase cell cycle arrest, and inhibits angiogenesis and endothelial cell proliferation. BAY-277 serves as a chemical probe for investigating the biological functions of METAP2. BAY-277 is applicable to cancer-related research.
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- Formule: C44H52N8O5
- Masse moléculaire:772.93
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
|
MetAp2 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | DC50 |
8.93 nM
Compound: EUB0003014
|
Degradation in HT1080 cells (CE) (Capillary electrophoresis (CE))
Degradation in HT1080 cells (CE) (Capillary electrophoresis (CE))
|
10.6019/CHEMBL5463725 |
| HUVEC | DC50 |
0.2 nM
Compound: EUB0003014
|
Degradation in HUVEC cells (WB) (Western Blot (WB))
Degradation in HUVEC cells (WB) (Western Blot (WB))
|
10.6019/CHEMBL5463725 |
| HUVEC | IC50 |
12 nM
Compound: EUB0003014
|
2D HUVEC cells proliferation assay
2D HUVEC cells proliferation assay
|
10.6019/CHEMBL5463725 |
In Vitro
BAY-277 degrades METAP2 in human umbilical vein endothelial cells (HUVEC) and HT1080 fibrosarcoma cells.
BAY-277 potently inhibits the enzymatic activity of recombinant human METAP2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 772.93
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Formule C44H52N8O5
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SMILES
O=C(N1CCC(C2=CC=C3C(CN(C4C(NC(CC4)=O)=O)C3=O)=C2)CC1)CCCCCN(CC5)CCC5C6=CC=C(C=C6)OC7=NN8C(C9=C7CCCC9)=NN=C8
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)