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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).

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PDK1-IN-RS2 Chemical Structure
PDK1-IN-RS2, CAS 1643958-89-7
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1 mL * 10 mM (in DMSO) 5 days $ 183.00
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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:(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

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences 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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Keywords

PDK1-IN-RS2 1643958-89-7 PI3K/Akt/mTOR signaling PDK PDK-1-IN-RS2 PDK1INRS2 PDK1 IN RS2 inhibitor inhibit

 

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