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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 329706-62-9
- 分子式: C30H23N5O4
- 分子量:517.53
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Eukaryotic Release Factor (eRF) アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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] |
体外実験
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.
化学情報
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CAS 番号 329706-62-9
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分子量 517.53
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AG6033 関連分類
HY-143435 関連分類
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