FL2-14
FL2-14 is a CRBN-dependent selective molecular glue degrader of GSPT2. FL2-14 specifically degrades GSPT2 by recruiting the CRBN E3 ligase to recognize the G-loop sequence on the target protein GSPT2. FL2-14 can be used in related research on colorectal cancer.
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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。
- 分子式: C27H25N5O8S
- 分子量:579.58
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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]|
eRF3b/GSPT2 |
体外実験
FL2-14 (10 μM; 16 h) downregulates the non-essential proteins GSPT2, FAM83F, and ZBTB39 in RKO WT cells, with preferential degradation of GSPT2. It loses the activity to degrade GSPT2 in RKO CRBN KO cells, indicating that its function is CRBN-dependent. It exhibits GSPT2-degrading activity in RKO cells stably overexpressing wild-type GSPT2 (GSPT2WT), but shows no degradation activity in cells overexpressing the GSPT2G566N mutant. It does not exert IKZF1-degrading activity in MV4.11 cells[1].
FL2-14 (1 nM-10 µM; 1-16 h) induces GSPT2 degradation in a concentration-dependent manner in RKO WT cells and HEK293T cells, and significant GSPT2 degradation is observed starting at 5 h post-treatment[1].
FL2-14 (1 nM-10 µM; 72 h) exhibits no significant cytotoxicity in RKO WT cells and HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:RKO WT, RKO CRBN KO, HEK293T cell lines
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Concentration:1 nM, 10 nM, 100 nM, 1 µM, 10 µM
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Incubation Time:1, 2, 3, 4, 5, 6, 8, 16 h
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Result:Significantly downregulated the protein levels of GSPT2, FAM83F, and ZBTB39, and preferentially degraded GSPT2.
Failed to degrade GSPT2, proving that its action was dependent on CRBN in RKO CRBN KO cells.
Induced the degradation of GSPT2 in a concentration-dependent manner.
Obviously induced the degradation of GSPT2 after 5 h of treatment.
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Cell Line:RKO cells stably overexpressing GSPT2WT or GSPT2G566N
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Concentration:10 μM
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Incubation Time:16 h
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Result:Successfully degraded wild-type GSPT2WT, but failed to degrade the G-loop mutated GSPT2G566N.
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Cell Line:MV4.11 cells
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Concentration:10 µM
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Incubation Time:16 h
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Result:Failed to induce the degradation of IKZF1.
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Cell Line:RKO WT and HEK293T cells
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Concentration:0.001, 0.01, 0.1, 1, 10 µM
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Incubation Time:72 h
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Result:Caused no significant cytotoxicity and did not significantly affect cell viability.
化学情報
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分子量 579.58
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分子式 C27H25N5O8S
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SMILES
O=C1C2=CC=C(NC3=CC=C(OS(N(C)CC4=NC=C(C5CC5)O4)(=O)=O)C=C3)C=C2C(N1C6C(NC(CC6)=O)=O)=O
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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)
FL2-14 関連分類
HY-177777 関連分類
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