2. Immunology/Inflammation Apoptosis Stem Cell/Wnt MAPK/ERK Pathway Cytoskeleton PI3K/Akt/mTOR
  3. PD-1/PD-L1 Apoptosis ERK JNK Cadherin p38 MAPK GSK-3 IFNAR Caspase Bcl-2 Family
  4. 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.

For research use only. We do not sell to patients.

SF-9-2

SF-9-2 Chemical Structure

CAS No. : 3053768-78-5

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SF-9-2 Related Antibodies

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GSK-3 GSK-3α GSK-3β

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

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Description

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[1].

IC50 & Target[1]

GSK-3β

 

Caspase 3

 

In Vitro

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.

SF-9-2 Related Antibodies

Cell Migration Assay [1]

Cell Line: SK-N-SH cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: SK-N-SH cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 24 h, 48 h
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.

Apoptosis Analysis[1]

Cell Line: SK-N-SH cells
Concentration: 1 μM, 3 μM, 6 μM
Incubation Time: 24 h
Result: Induced apoptosis, with the proportion of early and late apoptotic cells increasing in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: SK-N-SH cells
Concentration: 1 μM, 3 μM, 6 μM
Incubation Time: 24 h
Result: Increased the proportion of cells in the G1/S phase while decreasing the percentage of cells in the G2 phase.

Western Blot Analysis[1]

Cell Line: PD-L1 knockdown SK-N-SH cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 24 h
Result: Was weaker than that in normal SK-N-SH cells for the downregulation of ERK phosphorylation.

Immunofluorescence[1]

Cell Line: SK-N-SH cells
Concentration: 2.5 μM
Incubation Time: 24 h
Result: Reduced PD-L1 on the cell surface (red fluorescence) and internalized it into the cytoplasm as compound concentration increases.

ELISA Assay[1]

Cell Line: PBMCs
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 48 h
Result: Increased the secretion level of IFN-γ at 4 μM.
In Vivo

SF-9-2 (20-40 mg/kg, i.p., once a day, 21 days) suppresses SK-N-SH tumor growth in NOG mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SK-N-SH tumor (50 million cells/mL, s.c.) female NOG mice (5 weeks old, 17-20 g) model[1]
Dosage: 20 mg/kg, 40 mg/kg
Administration: i.p., once a day, 21 days
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.
Molecular Weight

515.55

Formula

C30H27F2N3O3
CAS No.
SMILES

N#CC1=CC(COC2=C(C=CC(OCC3=C(C(C4=CC=CC=C4F)=CC=C3)CF)=C2)CNCCO)=CN=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SF-9-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SF-9-23053768-78-5PD-1/PD-L1ApoptosisERKJNKCadherinp38 MAPKGSK-3IFNARCaspaseBcl-2 FamilyPD-1/Programmed death-ligand 1Extracellular signal regulated kinasesc-Jun N-terminal kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Interferon-α/β receptorInterferon-alpha/beta receptorInhibitorneuroblastomaSK-N-SH NOG mouseSK-N-SH cellsapoptosisMAPKinhibitorinhibit

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