SB1349
SB1349 is a potent Lin28 molecular glues degrader, with DC50 values of 1.594 µM and 0.777 µM for Lin28A and Lin28B, respectively. SB1349 induces proteasome-dependent degradation by directly binding and recruiting the E3 ubiquitin ligase RNF126. SB1349 can be used for the study of neuroblastoma.
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- Fòrmula: C34H31N5O8
- Peso molecular:637.64
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
IC50 & Target
[1]|
Lin28A 1.594 μM (DC50) |
Lin28B 0.777 μM (DC50) |
In Vitro
SB1349 (0.16-5 μM; 24 h) exerts a dose-dependent degradative effect on Lin28A and Lin28B proteins in JAR cells, with DC50 values of 1.594 µM and 0.777 µM, respectively; it dose-dependently upregulates mature let-7 miRNA levels and downregulates both the mRNA and protein levels of Lin28A, Lin28B, c-Myc and IMP1[1].
SB1349 (0.625-5 µM; 24-72 h) degrades Lin28B and Lin28A proteins in a dose-dependent manner in HEK293T and PA-1 cells, respectively; it exerts a dose-dependent degradative effect on Lin28B protein in SH-SY5Y cells[1].
SB1349 (1.25-5 µM; 72 h) promotes neuronal differentiation in SH-SY5Y cells, upregulates neuronal differentiation markers and downregulates the stemness marker (SOX2), induces morphological changes in cells, and significantly increases the total length and number of neurites[1].
SB1349 (5 µM; 24 h) loses the functions of degrading Lin28, downregulating target genes (c-Myc, IMP1), and upregulating let-7g in RNF126-knockdown JAR cells, indicating that its activity depends on RNF126[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:JAR, HEK293T, PA-1, and SH-SY5Y cells
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Concentration:0.16, 0.25, 0.31, 0.5, 0.625, 0.63, 1.25, 2.5, 5 µM
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Incubation Time:24 h, 72 h
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Result:Dose-dependently degraded Lin28A and/or Lin28B proteins across these cell lines.
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Cell Line:JAR cells
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Concentration:1.25, 2.5, 5 µM
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Incubation Time:24 h
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Result:Dose-dependently downregulated the mRNA and protein expression levels of the oncogenes c-Myc and IMP1, and downregulated the mRNA levels of Lin28 itself.
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Cell Line:SH-SY5Y cells
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Concentration:1.25, 2.5, 5 µM
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Incubation Time:72 h
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Result:Upregulated the expression of neuronal differentiation markers (Synaptophysin, MAP2, NSE, AChE) while downregulating the expression of the stemness marker (SOX2).
Chemical Information
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Peso molecular 637.64
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Fòrmula C34H31N5O8
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SMILES
COC1=CC=C(C=C1)C(/C=C/C(N2CCN(CC2)C3=CC4=C(C5=C(C(C)(O4)C)C=NN5C6=CC=C(C=C6)C(O)=O)C=C3[N+]([O-])=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)