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.
For research use only. We do not sell to patients.
- Formula: C34H31N5O8
- Molecular Weight:637.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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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Molecular Weight 637.64
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)