PDK1-IN-RS2

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PDK1-IN-RS2 

PDK1-IN-RS2 是一种肽对接基序 (PIFtide) 的模拟物，也是一种底物选择性 PDK1 抑制剂，Kd 为 9 μM。PDK1-IN-RS2 抑制 PDK1 对下游激酶 S6K1 的激活。

PDK1-IN-RS2

PDK1-IN-RS2 Chemical Structure

CAS No. : 1643958-89-7

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生物活性

PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1[1].

IC50 & Target

Kd: 9 μM (PDK1)[1]
体外研究
(In Vitro)

PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold. The sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge, because the sulfonamide is likely ionized under the crystallization conditions[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

380.89

Formula

C15H9ClN2O2S3
CAS 号

1643958-89-7
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.
参考文献

  • [1]. Rettenmaier TJ, et al. A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):18590-5.

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