TG100-115

产品说明书

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Chemical Structure| 677297-51-7 同义名 : -
CAS号 : 677297-51-7
货号 : A291714
分子式 : C18H14N6O2
纯度 : 98%
分子量 : 346.34
MDL号 : MFCD16038873
存储条件：

Pure form Keep in dark place, inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

5% DMSO+30% PEG 300+water 0.4 mg/mL

生物活性
靶点

  • p110β

    PI3Kβ, IC50:1.2 μM

  • p110δ

    PI3Kδ, IC50:235 nM

  • p110α

    PI3Kα, IC50:1.3 μM

  • p110γ

    PI3Kγ, IC50:83 nM
描述 TG100-115 effectively targets PI3Kγ and PI3Kδ, with IC50s of 83 nM and 235 nM, respectively, while showing minimal impact on PI3Kα and PI3Kβ (IC50 values >1 μM). In terms of specificity, TG100-115 was tested against a panel of 133 protein kinases and did not inhibit any at IC50 values <1 μM. TG100-115 strongly counteracts edema and inflammation, which are key factors in myocardial infarction, by inhibiting mediators like vascular endothelial growth factor and platelet-activating factor. Conversely, it does not affect endothelial cell mitogenesis, which is crucial for tissue repair following ischemic damage[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
HUVEC cells 10 μM Function assay Inhibition of VEGF-induced VE-cadherin phosphorylation in HUVEC cells by Western blot at 10 uM 17685602
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.89mL

0.58mL

0.29mL

14.44mL

2.89mL

1.44mL

28.87mL

5.77mL

2.89mL
参考文献

[1]Song C, Bae Y, et al. Identification of TG100-115 as a new and potent TRPM7 kinase inhibitor, which suppresses breast cancer cell migration and invasion. Biochim Biophys Acta. 2017 Apr;1861(4):947-957.

[2]Doukas J, Wrasidlo W, et al. Phosphoinositide 3-kinase gamma/delta inhibition limits infarct size after myocardial ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2006 Dec 26;103(52):19866-71.