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PI3K/Akt/mTOR signaling PDK PDK1-IN-RS2

PDK1-IN-RS2

Catalog No. T16450   CAS 1643958-89-7

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

PDK1-IN-RS2, CAS 1643958-89-7
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Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM).
Targets&IC50 PDK1 : ic50 (kd)9 μM,  
In vitro Because the sulfonamide is likely ionized under the crystallization conditions, the sulfonyl group of PDK1-IN-RS2 interacts with Arg131 through a salt bridge. PDK1-IN-RS2 stimulates the catalytic activity of PDK1 toward a peptide substrate by sixfold [1].
Molecular Weight 380.89
Formula C15H9ClN2O2S3
CAS No. 1643958-89-7

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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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