1. PI3K/Akt/mTOR
  2. PDK-1
  3. PS210

PS210 

Cat. No.: HY-121629
Handling Instructions

PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K.

For research use only. We do not sell to patients.

PS210 Chemical Structure

PS210 Chemical Structure

CAS No. : 1221962-86-2

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Description

PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K[1][2].

IC50 & Target

Kd: 3 μM (PDK1)[2]

In Vitro

When PS210 induces a stabilization of PDK1 to the temperature gradien, PS210 stabilized the residue Arg131, located opposite to the helix a-B at the other extreme of the helix a-C. Thus, the residues forming part of the phosphate-binding site appear to be a fixed point that allows for the relative movement of the helices in the process of PDK1 activation[1].

Molecular Weight

380.31

Formula

C₁₉H₁₅F₃O₅

CAS No.

1221962-86-2

SMILES

O=C(C(C(O)=O)C(CC(C1=CC=C(C=C1)C(F)(F)F)=O)C2=CC=CC=C2)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

PS210PS 210PS-210PDK-1Phosphoinositide dependent protein kinase-1PIF-bindingpocketArg131S6KPIFtideThr148Lys76helixa-BPS423Inhibitorinhibitorinhibit

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PS210
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