AG6033
AG6033 is a CRBN-dependent molecular glue degrader targeting GSPT1 (DC50 of 2.5 μM) and IKZF1. AG6033 induces degradation of GSPT1 via π-π stacking and hydrogen bonding with CRBN in a partially CRBN-dependent manner, decreases IKZF1 levels, and promotes degradation of CRBN substrates. AG6033 induces apoptosis in lung adenocarcinoma cells. AG6033 can be used for the research of lung cancer.
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- No. CAS: 329706-62-9
- Fòrmula: C30H23N5O4
- Peso molecular:517.53
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Almacenamiento:
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Ver todos los productos específicos de isoformas Eukaryotic Release Factor (eRF)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
eRF3a/GSPT1 2.5 μM (DC50) |
IKZF1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.853 μM
Compound: AG6033
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Antitumor activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
Antitumor activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTS assay
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[PMID: 35413617] |
In Vitro
AG6033 induces CRBN-dependent degradation of GSPT1 and IKZF1, inhibits A549 cell proliferation with an IC50 of 0.853 μM, and triggers apoptosis in A549 cells[1].
AG6033 (1-10 μM; 24 h) promotes apoptosis of human lung adenocarcinoma A549 cells in a concentration-dependent manner[2].
AG6033 (1.25-5 μM) induces degradation of the CRBN neosubstrates IKZF1 and GSPT1 in human lung adenocarcinoma A549, human multiple myeloma U266, and human acute myeloid leukemia OCI-AML2 cells, with no significant effect on CK1α levels[2].
AG6033 (1-31.6 μM; 48 h) exerts a cytotoxic effect on human multiple myeloma U266 cells that is CRBN-dependent, as CRBN knockout confers resistance to AG6033-induced viability loss[2].
AG6033 achieves structural matching with CRBN and binds via key π-π stacking interactions with TRP380, TRP386, TRP400, and HIS397, plus a hydrogen bond with GLU377[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human lung adenocarcinoma A549 cells
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Concentration:0.064 μM, 0.32 μM, 1.6 μM, 8 μM, 40 μM
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Incubation Time:48 h
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Result:Potently inhibited the viability of A549 cells, with an IC50 value of 0.853 μM.
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Cell Line:human lung adenocarcinoma A549 cells
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Concentration:1 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Increased the proportion of apoptotic A549 cells in a concentration-dependent manner.
At 1 μM, early and late apoptotic cells accounted for 5.66% and 5.39% of the population, respectively.
At 5 μM, early and late apoptotic cells accounted for 25.8% and 22.0% of the population, respectively.
At 10 μM, early and late apoptotic cells accounted for 36.2% and 29.1% of the population, respectively.
Induced apoptosis levels comparable to that induced by 1 μM doxorubicin at 5 μM.
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Cell Line:CRBN-knockout and control human multiple myeloma U266 cells
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Concentration:1 μM, 3.16 μM, 10 μM, 31.6 μM
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Incubation Time:48 h
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Result:Rendered CRBN-knockout U266 cells resistant, as shown by significantly higher cell viability in sg-CRBN cells compared to sg-NC cells at equivalent concentrations.
Chemical Information
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No. CAS 329706-62-9
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Peso molecular 517.53
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Fòrmula C30H23N5O4
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SMILES
O=C(N/N=C1C(N(CC(NC2=CC=CC=C2)=O)C3=C\1C=CC=C3)=O)C4=CC=CC(NC(C5=CC=CC=C5)=O)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AG6033 Related Classifications
HY-143435 Related Classifications
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