1. GPCR/G Protein
  2. G Protein-coupled Receptor Kinase (GRK)
  3. GRK5-IN-5

GRK5-IN-5 (Compound 4a) 是一种选择性的 G 蛋白偶联受体激酶 5 (GRK5) 抑制剂,其 IC50 值为 0.03 μM。GRK5-IN-5 对 GRK2 和 GRK6 的 IC50 值为 2.2 和 0.036 μM。GRK5-IN-5 具有强效的抗心肌肥厚活性,还能抑制非心肌细胞的增殖。GRK5-IN-5 可抑制肥厚标志物基因 Nppa 和 Nppb 的异常上调,从而阻断病理性心肌重构。GRK5-IN-5 可用于心肌肥厚的研究。

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GRK5-IN-5

GRK5-IN-5 Chemical Structure

CAS No. : 3061801-11-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy[1].

IC50 & Target[1]

GRK5

0.03 μM (IC50)

GRK6

0.036 μM (IC50)

GRK2

2.2 μM (IC50)

分子量

542.56

Formula

C30H27FN4O5

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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产品名称:
GRK5-IN-5
目录号:
HY-180583
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