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1643958-89-7

1643958-89-7 structure
1643958-89-7 structure
  • Name: PDK1-IN-RS2
  • Chemical Name: PDK1-IN-RS2
  • CAS Number: 1643958-89-7
  • Molecular Formula: C15H9ClN2O2S3
  • Molecular Weight: 380.89
  • Catalog: Signaling Pathways PI3K/Akt/mTOR PDK-1
  • Create Date: 2020-04-11 14:34:18
  • Modify Date: 2024-01-15 11:22:33
  • 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].

Name PDK1-IN-RS2
Description 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].
Related Catalog
Target

Kd: 9 μM (PDK1)[1]

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].
References

[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.

Molecular Formula C15H9ClN2O2S3
Molecular Weight 380.89