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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- Fòrmula: C27H25N5O8S
- Peso molecular:579.58
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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]|
eRF3b/GSPT2 |
In Vitro
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.
Chemical Information
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Peso molecular 579.58
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Fòrmula 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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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)
FL2-14 Related Classifications
HY-177777 Related Classifications
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