1. Immunology/Inflammation
  2. PD-1/PD-L1
  3. PD-1/PD-L1-IN-61

PD-1/PD-L1-IN-61 是一种 PD-1/PD-L1 相互作用抑制剂,对人源的 IC50 为 5.3 nM。PD-1/PD-L1-IN-61 可嵌入 PD-L1 二聚体界面的疏水口袋,通过与 PD-L1 残基形成氢键和 π-π 堆积作用稳定结合。PD-1/PD-L1-IN-61 可作为免疫激活剂,增强外周血单个核细胞对癌细胞的免疫杀伤活性,恢复 T 细胞 的免疫功能,并促进 IFN-γ 分泌。PD-1/PD-L1-IN-61 可用于三阴性乳腺癌的相关研究。

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PD-1/PD-L1-IN-61

PD-1/PD-L1-IN-61 Chemical Structure

CAS No. : 2983098-90-2

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  • 生物活性

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生物活性

PD-1/PD-L1-IN-61 is a PD-1/PD-L1 interaction inhibitor with a human IC50 of 5.3 nM. PD-1/PD-L1-IN-61 embeds into the hydrophobic pocket at the PD-L1 dimer interface, stabilizing binding through hydrogen bonds and π-π stacking with PD-L1 residues. PD-1/PD-L1-IN-61 acts as an immune activator, enhances immune-killing activity of peripheral blood mononuclear cells against cancer cells, restores T-cell immune function, and promotes IFN-γ secretion. PD-1/PD-L1-IN-61 can be used for the research of triple-negative breast cancer[1].

体外研究
(In Vitro)

PD-1/PD-L1-IN-61 (III-4) (1-16 μM) 对 MDA-MB-231 和 Jurkat 细胞仅表现出极微弱的细胞毒性[1]
PD-1/PD-L1-IN-61 (0.5-2 μM) 可呈剂量依赖性增强 PBMC 介导的 MDA-MB-231 细胞杀伤作用,在 1 μM 时诱导 38.4% 的肿瘤细胞杀伤[1]
PD-1/PD-L1-IN-61 (10-1000 nM) 呈剂量依赖性促进人外周血单个核细胞 (hPBMCs) 分泌 IFN-γ,在 100 nM 和 1000 nM 浓度下分泌量显著升高[1]

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

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231 and Jurkat cells
Concentration: 1, 2, 4 ,8, 16 μM
Incubation Time: null
Result: Showed negligible cytotoxicity against MDA-MB-231 and Jurkat cells in a CCK-8 assay.
分子量

776.83

Formula

C42H44N6O9

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
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  • 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.

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产品名称:
PD-1/PD-L1-IN-61
目录号:
HY-182047
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