2. Metabolic Enzyme/Protease TGF-beta/Smad Immunology/Inflammation NF-κB MAPK/ERK Pathway
  3. NADPH Oxidase TGF-β Receptor Reactive Oxygen Species (ROS) p38 MAPK
  4. GK-136901

GK-136901 是一种口服有效的、双重 Nox1/Nox4 NADPH 氧化酶抑制剂，对 Nox1 的 Ki=160 nM，Nox4 的 Ki=165 nM。GK-136901 有效阻断高糖诱导的肾细胞内活性氧生成、p38-MAPK 磷酸化以及 TGF-β1/2 和纤连蛋白 (fibronectin) 的上调。GK-136901 同时抑制低氧环境下小鼠肺血管细胞的增殖。凭GK-136901 可用于 2 型糖尿病肾病、高糖相关肾脏病变及肺动脉高压发病机制的研究。

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GK-136901

GK-136901 Chemical Structure

CAS No. : 1062624-71-8

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GK-136901 相关抗体

Top Publications Citing Use of Products

查看 NADPH Oxidase 亚型特异性产品:

查看所有亚型
NOX1 NOX2 NOX4 NOX5 DUOX1

查看 TGF-β Receptor 亚型特异性产品:

查看所有亚型
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GK-136901 is an orally active, dual Nox1/Nox4 NADPH oxidase inhibitor with a Ki of 160 nM for Nox1 and 165 nM for Nox4. GK-136901 potently blocks high glucose-induced intracellular reactive oxygen species production, p38-MAPK phosphorylation, and upregulation of TGF-β1/2 and fibronectin (fibronectin) in renal cells. GK-136901 also inhibits the proliferation of mouse pulmonary vascular cells under hypoxic conditions. GK-136901 is applicable to the research on the pathogenesis of type 2 diabetic nephropathy, high glucose-related renal lesions and pulmonary hypertension[1][2][3][4].

IC50 & Target

NOX4

165 nM (Ki)

NOX1

160 nM (Ki)

体外研究
(In Vitro)

GKT136901 (10 μM；30 分钟) 可抑制高 D-葡萄糖诱导的 MPT 细胞中 NADPH 氧化酶活性及 ROS 生成[2]。
GKT136901 (10 μM；30 分钟) 可抑制高 D-葡萄糖诱导的 MPT 细胞中促纤维化蛋白的表达以及 p38MAP 激酶活化[2]。

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

GK-136901 相关抗体:

Western Blot Analysis[2]

Cell Line: Immortalized mouse proximal tubule (MPT) cells
Concentration: 10 μM
Incubation Time: 30 min pre-incubation; 2 hr high D-glucose exposure
Result: Abolished high D-glucose-induced phosphorylation of p38MAP kinase.
Showed no significant effect on p38MAP kinase phosphorylation when used alone or in combination with high L-glucose.

Western Blot Analysis[2]

Cell Line: Immortalized mouse proximal tubule (MPT) cells
Concentration: 10 μM
Incubation Time: 30 min pre-incubation; high D-glucose exposure
Result: Inhibited high D-glucose-induced increases in TGF-β1/2 protein expression.
Inhibited high D-glucose-induced increases in fibronectin protein expression.
体内研究
(In Vivo)

GK-136901 可减轻肺动脉高压小鼠模型中缺氧诱导的肺血管细胞增殖[4]。
GK-136901 在小鼠体内耐受性良好，经口给药剂量已测试至 1000 mg/kg[5]。

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

346.38

Formula

C20H18N4O2
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

GK-136901 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:

GK-1369011062624-71-8GK136901GK 136901NADPH OxidaseTGF-β ReceptorReactive Oxygen Species (ROS)p38 MAPKNOXTransforming growth factor beta receptorsNADPH oxidaseTGF-β1/2fibronectinp38MAP kinaseNox4pulmonary hypertensionNox1MPT cellskidney cellstype 2 diabetic nephropathyInhibitorinhibitorinhibit

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