1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. DGK Interleukin Related
  3. DGKα-IN-10

DGKα-IN-10 是一种具有口服活性的强效 DGKα 抑制剂,其 IC50 为 0.27 nM。DGKα-IN-10 可诱导 IL-2 释放和 T 细胞增殖。DGKα-IN-10 可用于癌症研究,如结肠癌。

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DGKα-IN-10

DGKα-IN-10 Chemical Structure

CAS No. : 2980579-79-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DGKα-IN-10 is an orally active and potent DGKα inhibitor with an IC50 of 0.27 nM. DGKα-IN-10 can induce IL-2 release and T cells proliferation. DGKα-IN-10 can be used for the research of cancer, such as colon cancer[1].

IC50 & Target[1]

DKGα

0.27 nM (IC50)

IL-2

 

体外研究
(In Vitro)

DGKα-IN-10 (Compound 16) 可诱导人外周血单个核细胞 (PBMCs) 中 IL-2 的释放,其 EC50 值为 0.29 μM[1]
DGKα-IN-10 (12-1000 nM, 4 h) 可促进 PBMCs 中 CD4+ 和 CD8+ T 细胞的增殖[1]
DGKα-IN-10 (59.85-163.3 nM) 能增强人 T 细胞中 pERK 的激活[1]
DGKα-IN-10 (1 μM) 对 DGKα 的选择性比对大多数 DGK 同工型高 100 倍[1]

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

Cell Proliferation Assay[1]

Cell Line: Human peripheral blood mononuclear cells (PBMCs)
Concentration: 12, 37, 111, 333 and 1000 nM
Incubation Time: 4 h
Result: Increased CD4+ and CD8+ T cells.
体内研究
(In Vivo)

DGKα-IN-10 (Compound 16) (0.5-10 mg/kg,口服,每日两次) 与抗 PD-1 抗体联合使用时,可抑制 MC38/CT26 异种移植 C57BL/6J 小鼠的肿瘤生长[1]

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

Animal Model: MC38/CT26 xenograft C57BL/6J mice models[1]
Dosage: 0.5, 3 and 10 mg/kg, combined with anti-PD-1 antibody (3-5 mg/kg)
Administration: Orally administration, twice a day
Result: Reduced tumor volume.
Showed tumor growth inhibition (TGI) rate of 51.2%-90.3%.
Had no significant body weight loss.
分子量

459.50

Formula

C25H25N5O4

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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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.

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产品名称:
DGKα-IN-10
目录号:
HY-178062
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