SF-9-2
SF-9-2 is a PD-L1/PD-1 binding inhibitor (IC50 = 24.9 nM). SF-9-2 inhibits epithelial-mesenchymal transition, migration, invasion, and proliferation of SK-N-SH cells, and also induces apoptosis and cell cycle arrest. SF-9-2 blocks PD-L1-induced SK-N-SH cell growth through the MAPK signaling pathway. SF-9-2 restores GSK-3β activity and enhances PD-L1 degradation through the ubiquitin-proteasome pathway. SF-9-2 inhibits tumor growth in the SK-N-SH NOG mouse model without significant toxicity. SF-9-2 also acts as an immune checkpoint inhibitor, blocking PD-L1 to restore T cell function. SF-9-2 can be used in neuroblastoma research.
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- CAS No.: 3053768-78-5
- 화학식: C30H27F2N3O3
- 분자량:515.55
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Biological Activity
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GSK-3β |
Caspase 3 |
SF-9-2 (0.5-16 μM, 48 h) exhibits significant inhibitory activity against SK-N-SH (IC50 = 5.9 μM) and SK-N-AS cells (IC50 = 8.67 μM) but has minimal inhibitory effects on SH-SY5Y and SK-N-BE (2) cells, and exhibits weak cytotoxic effects on normal cell MRC-5 (IC50 = 12.15 μM)[1].
SF-9-2 (1-6 μM, 24 h) inhibits the proliferation, migration, invasion and epithelial-mesenchymal transition (EMT), and induces mitochondria-dependent apoptosis and cell cycle arrest in SK-N-SH cells[1].
SF-9-2 (2.5-8 μM, 24-48 h) inhibits the MAPK pathway and downregulates PD-L1 Levels through targeting the ERK signaling pathway in SK-N-SH Cells[1].
SF-9-2 (2.5-5 μM, 24 h) induces PD-L1 internalization and proteasomal degradation mediated by GSK-3βin SK-N-SH Cells[1].
SF-9-2 (2.25-200 nM) decreases the fluorescence signal, effectively blocking the PD-1/PD-L1 immune checkpoint in 293T cells overexpressing PD-1 and Fc-PD-L1 protein[1].
SF-9-2 (1-16 μM, 48 h) increased the secretion level of IFN-γ in PBMCs and shows no obvious toxicity to PBMCs at concentrations of 1, 2, and 4 μM[1].
SF-9-2 (1-8 μM, 48 h) can exhibit both direct tumoricidal activity and T cell-mediated cytotoxicity against SK-N-SH cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-SH cells
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Concentration:1 μM, 2 μM, 4 μM
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Incubation Time:24 h
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Result:Inhibited the migration, reduced the number of cells passing through the chamber, with the migration rate in the 1, 2, 4 μM group was 73.3%, 43.0%, 13.4%, respectively.
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Cell Line:SK-N-SH cells
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Concentration:2.5 μM, 5 μM
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Incubation Time:24 h, 48 h
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Result:Up-regulated the expressions of N-cadherin and E-cadherin, and down-regulated the expressions of β-catenin, and vimentin.
Reduced the Bcl-2/BAX ratio and increased the cleavage of Caspase 3.
Reduced the phosphorylation levels of ERK and JNK, and increased the phosphorylation level of p38 at 48 h.
Reduced PD-L1 levels at 5 μM.
Reduced the level of p-GSK-3β (Ser9), weakened the inhibitory effect of p-ERK on GSK-3β to a certain extent, and promoted the activation of GSK-3β at 5 μM.
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Cell Line:SK-N-SH cells
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Concentration:1 μM, 3 μM, 6 μM
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Incubation Time:24 h
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Result:Induced apoptosis, with the proportion of early and late apoptotic cells increasing in a dose-dependent manner.
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Cell Line:SK-N-SH cells
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Concentration:1 μM, 3 μM, 6 μM
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Incubation Time:24 h
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Result:Increased the proportion of cells in the G1/S phase while decreasing the percentage of cells in the G2 phase.
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Cell Line:PD-L1 knockdown SK-N-SH cells
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Concentration:2.5 μM, 5 μM
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Incubation Time:24 h
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Result:Was weaker than that in normal SK-N-SH cells for the downregulation of ERK phosphorylation.
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Cell Line:SK-N-SH cells
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Concentration:2.5 μM
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Incubation Time:24 h
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Result:Reduced PD-L1 on the cell surface (red fluorescence) and internalized it into the cytoplasm as compound concentration increases.
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Cell Line:PBMCs
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Concentration:1 μM, 2 μM, 4 μM
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Incubation Time:48 h
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Result:Increased the secretion level of IFN-γ at 4 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SK-N-SH tumor (50 million cells/mL, s.c.) female NOG mice (5 weeks old, 17-20 g) model[1]
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Dosage:20 mg/kg, 40 mg/kg
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Administration:i.p., once a day, 21 days
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Result:Inhibited tumor growth, with tumor inhibition rates of 23.79% (20 mg/kg) and 69.45% (40 mg/kg) respectively.
Had no effects on body weight or mortality, exhibited no apparent nephrotoxicity or hepatotoxicity.
Chemical Information
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CAS No. 3053768-78-5
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분자량 515.55
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화학식 C30H27F2N3O3
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SMILES
N#CC1=CC(COC2=C(C=CC(OCC3=C(C(C4=CC=CC=C4F)=CC=C3)CF)=C2)CNCCO)=CN=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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