2. Immunology/Inflammation Apoptosis MAPK/ERK Pathway Stem Cell/Wnt 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 是一种 PD-L1/PD-1 结合抑制剂 (IC50 = 24.9 nM)。SF-9-2 抑制了 SK-N-SH 细胞的上皮间质转化、迁移、侵袭和增殖，还诱导其凋亡 (apoptosis) 和细胞周期停滞。SF-9-2 通过 MAPK 信号通路阻断 PD-L1 诱导的 SK-N-SH 细胞生长。SF-9-2 恢复 GSK-3β 活性，并通过泛素-蛋白酶体通路增强 PD-L1 降解。SF-9-2 抑制了 SK-N-SH NOG 小鼠模型中的肿瘤生长，且无明显毒性。SF-9-2 还可作为免疫检查点抑制剂，阻断 PD-L1 以恢复 T 细胞功能。SF-9-2 可用于神经母细胞瘤研究。

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SF-9-2

SF-9-2 Chemical Structure

CAS No. : 3053768-78-5

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SF-9-2 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

SF-9-2 (0.5-16 μM, 48 小时) 对 SK-N-SH (IC50 = 5.9 μM) 和 SK-N-AS 细胞 (IC50 = 8.67 μM) 表现出显著的抑制活性，但对 SH-SY5Y 和 SK-N-BE (2) 细胞的抑制作用较小，对正常细胞 MRC-5 (IC50 = 12.15 μM) 表现出较弱的细胞毒性作用[1]。
SF-9-2 (1-6 μM, 24 小时) 可抑制 SK-N-SH 细胞增殖、迁移、侵袭和上皮-间质转化 (EMT)，并诱导其发生线粒体依赖性细胞凋亡和细胞周期停滞[1]。
SF-9-2 (2.5-8 μM, 24-48 小时) 可通过靶向 ERK 信号通路抑制 SK-N-SH 细胞中的 MAPK 通路并下调 PD-L1 水平[1]。
SF-9-2 (2.5-5 μM, 24 小时) 诱导 SK-N-SH 细胞中 GSK-3β 介导的 PD-L1 内化和蛋白酶体降解[1]。
SF-9-2 (2.25-200 nM) 在过表达 PD-1 和 Fc-PD-L1 蛋白的 293T 细胞中可降低荧光信号，有效阻断的 PD-1/PD-L1 免疫检查点[1]。
SF-9-2 (1-16 μM, 48 小时) 可提高 PBMCs 中 IFN-γ 的分泌水平，在 1、2 和 4 μM 浓度下对 PBMCs 无明显毒性[1]。
SF-9-2 (1-8 μM, 48 小时) 可表现出直接的肿瘤杀伤活性和 T 细胞介导的针对 SK-N-SH 细胞的细胞毒作用[1]。

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

SF-9-2 相关抗体:

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.
体内研究
(In Vivo)

SF-9-2 (20-40 mg/kg，腹腔注射，每天一次，21 天) 抑制 NOG 小鼠模型中的 SK-N-SH 肿瘤生长[1]。

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.
分子量

515.55

Formula

C30H27F2N3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SF-9-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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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