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PHT-427

Cat No.
CEI-0103
Description
PHT-427
CAS No.
1191951-57-1
Molecular Weight
409.61
Purity
>99%
Storage
2 years at -20 centigrade
Targets
Akt, PDPK1
Molecular Formula
C20H31N3O2S2
Solubility
No
In vitro
PHT-427 can inhibit both Akt and PDPK1 with Ki values of 2.7 uM and 5.2 uM. PHT-427 itself (C-12 chain) bound with the highest affinity to the PH domains of both PDPK1 and Akt. PHT-427 inhibited Akt and PDKP1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. The PDPK1-independent phospho-Ser473-Akt was slightly increased by PHT-427, but completely inhibited in by wortmannin. Phospho-Ser657-protein kinase C (PKC) and total SGK1 are decreased by treatment with both PHT-427 and wortmannin. In the BxPC-3 cells which is sensitive to the antitumor activity of PHT-427, shows a decrease of both phospho-Ser473-Akt and phospho-Thr308-Akt.
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