1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. PS315

PS315 

Cat. No.: HY-124308
Handling Instructions

PS315, a derivative of PS48, is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCι (IC50=30 μM). PS315 has anti-cancer activity.

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

PS315 Chemical Structure

PS315 Chemical Structure

CAS No. : 1221964-50-6

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Description

PS315, a derivative of PS48, is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCι (IC50=30 μM). PS315 has anti-cancer activity[1].

IC50 & Target

PKCζ

10 μM (IC50)

PKCη

30 μM (IC50)

In Vitro

Preincubation of U937 cells with 5 μM PS315 inhibits TNF-α induced NF-κB activation by 74%, whereas complete inhibition is observed with 10 μM PS315[1].
The small allosteric inhibitor PS315 and the N-terminal region of aPKC both act directly on the PIF-pocket on-off switch. PS315, binding at the PIF-pocket, induces a displacement of the active site residue Lys111, thereby inhibiting the activity of aPKCs by allosterically affecting the catalytic mechanism of the kinase[1].

Molecular Weight

362.85

Formula

C₂₃H₁₉ClO₂

CAS No.

1221964-50-6

SMILES

O=C(O)/C=C(C1=CC=C(C2=CC=CC=C2)C=C1)/CCC3=CC=C(Cl)C=C3

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Storage

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

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Keywords:

PS315PS 315PS-315PKCProtein kinase CPS48allostericPIF-pocketaPKCdisplacementLys111full-lengthcatalyticdomainanti-cancerInhibitorinhibitorinhibit

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PS315
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HY-124308
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