PS315
PS315, a derivative of PS48 (HY-15967), 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 PKCη (IC50=30 μM). PS315 has anti-cancer activity.
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- CAS No.: 1221964-50-6
- Formule: C23H19ClO2
- Masse moléculaire:362.85
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PKCζ 10 μM (IC50) |
PKCη 30 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1221964-50-6
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Masse moléculaire 362.85
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Formule C23H19ClO2
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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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PS315 Related Classifications
HY-124308 Related Classifications
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