1. Immunology/Inflammation PI3K/Akt/mTOR
  2. PD-1/PD-L1 IFNAR Interleukin Related PI3K Akt
  3. PD-1/PD-L1-IN-54

PD-1/PD-L1-IN-54 (Compound 6) 是一种中等亲和力的 PD-1/PD-L1 抑制剂 (KD: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC50: 88.6 μM)。其抑制 PD-1/PD-L1 相互作用,且通过激活 CD8+ T 细胞,上调 PD-1 表达和提高 IFN-γI IL-2 的分泌展现出抗癌活性。PD-1/PD-L1-IN-54 抑制癌细胞增殖并促进凋亡 (Apoptosis)。PD-1/PD-L1-IN-54 也通过与 PD-1/PD-L1 相关的 PI3K/Akt 通路调节 T 细胞免疫。

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PD-1/PD-L1-IN-54 Chemical Structure

PD-1/PD-L1-IN-54 Chemical Structure

CAS No. : 1393644-68-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PD-1/PD-L1-IN-54 (Compound 6) is a moderately affinic PD-1/PD-L1 inhibitor (KD: PD-1, 55.8 μM; PD-L1, 46.4 μM; IC50: 88.6 μM). PD-1/PD-L1-IN-54 inhibits PD-1/PD-L1 interactions and shows anticancer activity by activating CD8+ T cells, upregulating PD-1 expression, and increasing secretion of IFN-γ and IL-2. PD-1/PD-L1-IN-54 inhibits cancer cell proliferation and promotes apoptosis. PD-1/PD-L1-IN-54 also regulates T cell immunity through the PI3K/Akt pathway correlated with PD-1/PD-L1[1].

IC50 & Target[1]

IL-2

 

PI3K

 

Akt

 

体外研究
(In Vitro)

PD-1/PD-L1-IN-54 (15-60 μM, 48 h) 可促进 CD8+ T 细胞的增殖并抑制肿瘤细胞 (LLC 和 MC38) 的生长[1]
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) 促进共培养系统中 CD8+ T 细胞分泌免疫细胞因子(IFN-γ 和 IL-2),并促进肿瘤细胞 (LLC 和 MC38) 的凋亡[1]
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) 促进与 LLC 或 MC38 细胞共培养的 CD8+ T 细胞中 PD-1 表达[1]
PD-1/PD-L1-IN-54 (15-60 μM, 48 h) 调节 PD-1/PD-L1 相互作用的下游通路 (PI3K/Akt)[1]

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

Western Blot Analysis[1]

Cell Line: Co-culture system consisting of activated CD8+ T cells and tumor cells (LLC or MC38) added in a 5:1 ratio
Concentration: 15, 30, 60 μM
Incubation Time: 48 h
Result: Promoted phosphorylation of PI3K, Akt and NF-κB in T cells

Cell Viability Assay[1]

Cell Line: Co-culture system consisting of activated CD8+ T cells and tumor cells (LLC or MC38) added in a 5:1 ratio
Concentration: 15, 30, 60 μM
Incubation Time: 48 h
Result: Inhibited the proliferation of LLC and MC38 tumor cells and stimulated the proliferation of CD8+ T cells
分子量

368.77

Formula

C17H17ClO7

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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PD-1/PD-L1-IN-54
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HY-159892
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