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
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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 | |
| 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 |
| Molecular Formula | C23H19ClO2 |
|---|---|
| Molecular Weight | 362.85 |