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 PKC_ζ (IC₅₀=10 μM) and PKC_η (IC₅₀=30 μM). PS315 has anti-cancer activity^[1].

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.

362.85

C₂₃H₁₉ClO₂

1221964-50-6

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. Zhang H, et al. Molecular mechanism of regulation of the atypical protein kinase C by N-terminal domains and an allosteric small compound. Chem Biol. 2014 Jun 19;21(6):754-65.  [Content Brief]