2. Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Indoleamine 2,3-Dioxygenase (IDO) Interleukin Related Apoptosis Caspase PARP
  4. IDO1-IN-34

IDO1-IN-34 是一种选择性 IDO1 抑制剂，IC50 为 0.093 μM。IDO1-IN-34 对多种癌细胞系具有细胞毒性。IDO1-IN-34 可抑制犬尿氨酸 (kynurenine) 通路、激活 IL-2。IDO1-IN-34 通过内源性线粒体通路诱导细胞凋亡 (apoptosis)，同时使细胞色素 c (cytochrome c)、caspase-3、caspase-9 和 PARP-1 水平升高。IDO1-IN-34 可用于肝癌、肺癌、乳腺癌、前列腺癌、结肠癌、白血病的研究。

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IDO1-IN-34

IDO1-IN-34 Chemical Structure

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Customer Review

IDO1-IN-34 相关抗体

Top Publications Citing Use of Products

查看 Indoleamine 2,3-Dioxygenase (IDO) 亚型特异性产品:

查看所有亚型
IDO1 IDO2 IDO

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IDO1-IN-34 is a selective IDO1 inhibitor with an IC50 of 0.093 μM. IDO1-IN-34 exhibits cytotoxicity against various cancer cell lines. IDO1-IN-34 inhibits the kynurenine (kynurenine) pathway and activates IL-2. IDO1-IN-34 induces cell apoptosis via the endogenous mitochondrial pathway, while increasing the levels of cytochrome c, caspase-3, caspase-9 and PARP-1. IDO1-IN-34 can be used for research on liver cancer, lung cancer, breast cancer, prostate cancer, colon cancer and leukemia[1].

IC50 & Target[1]

IDO1

0.093 μM (IC50)

IL-2

 

Caspase-9

 

Caspase-3

 

PARP-1

 

体外研究
(In Vitro)

IDO1-IN-34 (Compound 3b) (0.1-100 μM; 48 h) 对多种癌细胞系具有选择性细胞毒性，对 HepG2 细胞的效力最高 (GI50 = 0.72 μM)，对非癌变 Vero 细胞的细胞毒性极低，针对 HepG2 细胞的选择性指数达 121.58[1]。
IDO1-IN-34 (0.03-0.3 μM; 24 h) 可剂量依赖性降低 IFN-γ 刺激的 SK-OV-3 细胞中犬尿氨酸的生成，逆转 IDO1 介导的免疫抑制[1]。
IDO1-IN-34 (0.03-0.3 μM; 2 days) 可在 IDO1 抑制的 SK-OV-3/Jurkat T 细胞共培养体系中，以剂量依赖的方式恢复 T 细胞活化，提高 IL-2 的表达[1]。
IDO1-IN-34 (0.36-0.72 μM; 24 h) 可剂量依赖性地诱导 HepG2 细胞凋亡[1]。
IDO1-IN-34 (0.36-0.72 μM; 48 h) 可剂量依赖性激活 HepG2 细胞中的内源性线粒体凋亡通路，表现为剪切型 caspase-3、剪切型 caspase-9、剪切型 PARP-1 和细胞色素 c 的水平升高，且不会激活外源性通路标志物剪切型 caspase-8[1]。

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

IDO1-IN-34 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HepG2, A549, MCF-7, PC-3, HT-29, K562, Vero
Concentration: 0.1-100 μM
Incubation Time: 48 h
Result: Exhibited a GI50 of 0.72 μM against HepG2 liver cancer cells.
Exhibited a GI50 of 3.02 μM against A549 lung cancer cells.
Exhibited a GI50 of 4.55 μM against MCF-7 breast cancer cells.
Exhibited a GI50 of 3.28 μM against PC-3 prostate cancer cells.
Exhibited a GI50 of 6.04 μM against HT-29 colon cancer cells.
Exhibited a GI50 of 10.27 μM against K562 leukemia cells.
Exhibited a GI50 of 87.54 μM against non-cancerous Vero cells.
Yielded selectivity indices of 121.58 (HepG2), 28.98 (A549), 19.23 (MCF-7), 26.68 (PC-3), 14.49 (HT-29), and 8.52 (K562).

ELISA Assay[1]

Cell Line: SK-OV-3/Jurkat T-cell co-cultures
Concentration: 0.03, 0.1, 0.3 μM
Incubation Time: 2 days
Result: Increased IL-2 levels to 416.59 pg/mL at 0.03 μM compared to 161.03 pg/mL in IFN-γ-only treated co-cultures.
Increased IL-2 levels to 648.84 pg/mL at 0.1 μM compared to 161.03 pg/mL in IFN-γ-only treated co-cultures.
Increased IL-2 levels to 865.67 pg/mL at 0.3 μM compared to 161.03 pg/mL in IFN-γ-only treated co-cultures.

Apoptosis Analysis[1]

Cell Line: HepG2 liver cancer cells
Concentration: 0.36 μM, 0.72 μM
Incubation Time: 24 h
Result: Increased total apoptosis (early + late) to 36.16% at 0.36 μM compared to 9.13% in control cells.
Increased total apoptosis (early + late) to 59.33% at 0.72 μM compared to 9.13% in control cells.

Western Blot Analysis[1]

Cell Line: HepG2 liver cancer cells
Concentration: 0.36 μM, 0.72 μM
Incubation Time: 48 h
Result: Dose-dependently increased levels of cytochrome c, cleaved caspase-3, cleaved caspase-9, and cleaved PARP-1.
Dose-dependently reduced levels of total caspase-3, total caspase-9, and total PARP-1.
Did not increase cleaved caspase-8 levels at either concentration tested.
分子量

527.19

Formula

C18H10BrF7N4O2
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

IDO1-IN-34 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

IDO1-IN-34Indoleamine 2,3-Dioxygenase (IDO)Interleukin RelatedApoptosisCaspasePARPILpoly ADP ribose polymerasekynurenine pathwayintrinsic mitochondrial pathwayIL-2HepG2 cellscaspase-9caspase-3cytochrome cPARP-1IDO1SK-OV-3 cellsInhibitorinhibitorinhibit

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