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PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity. PS315 is a derivative of PS48 and is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing displacement of the active site residue Lys111.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,520 | 6-8 weeks | |
50 mg | $1,980 | 6-8 weeks | |
100 mg | $2,500 | 6-8 weeks |
Description | PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity. PS315 is a derivative of PS48 and is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing d |
Targets&IC50 | PKCζ:10 μM, PKCη:30 μM |
In vitro | PS315, by attaching to the PIF-pocket, prompts a shift in the active site residue Lys111, effectively inhibiting aPKCs through an allosteric impact on the enzyme's catalytic process. A pre-treatment of U937 cells with 5 μM PS315 results in a 74% reduction in TNF-α-induced NF-κB activation, with total inhibition achieved at 10 μM PS315. The allosteric inhibitor PS315, along with the N-terminal region of aPKC, directly influences the PIF-pocket on-off switch[1]. |
Molecular Weight | 362.85 |
Formula | C23H19ClO2 |
Cas No. | 1221964-50-6 |
Relative Density. | 1.212 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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