1221964-50-6

1221964-50-6 structure

Name: PS315
Chemical Name: PS315
CAS Number: 1221964-50-6
Molecular Formula: C₂₃H₁₉ClO₂
Molecular Weight: 362.85
Catalog: Signaling Pathways Epigenetics PKC
Create Date: 2020-04-08 17:42:19
Modify Date: 2024-01-10 19:18:31
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[1].

Name	PS315

Description	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[1].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Research Areas >> Cancer Signaling Pathways >> TGF-beta/Smad >> PKC
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].
References	[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.

Molecular Formula	C₂₃H₁₉ClO₂
Molecular Weight	362.85