| Bioactivity | PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of 2.7 µM and 5.2 µM and for Akt and PDPK1, respectively. | ||||||||||||
| Invitro | The effects of PHT-427 on cell signaling are investigated by RPPA using a panel of 86 antibodies to phospho- and non-phosphorylated signaling protein related to PtdIns-3-K/PDPK1/Akt signaling in PC-3 prostate cells where PtdIns-3-K/PDPK1/Akt signaling is activated because of homozygous PTEN mutation. After 16 hours, a reduction is observed in phospho-Ser241-PDPK1 phospho-Thr308-Akt by both 10 µM PH-427 and 0.1 µM Wortmannin. Finally, phospho-Ser657-protein kinase C (PKC) and total SGK1 are decreased by treatment with both PHT-427 and Wortmannin. These results suggest that at 10 µM PHT-427 inhibits both Akt and PDKP1. The BxPC-3 and MiaPaCa-2 pancreatic cancer cell lines are probed by Western blotting following up to 24 hr exposure to 10 µM PHT-427, which is below the IC50 for cell growth inhibition of around 30 µM, to determine the effects of PHT-427 on of the PtdIns-3-K/PDPK1/Akt signaling pathway components[1]. | ||||||||||||
| Name | PHT-427 | ||||||||||||
| CAS | 1191951-57-1 | ||||||||||||
| Formula | C20H31N3O2S2 | ||||||||||||
| Molar Mass | 409.61 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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PHT-427
CAS: 1191951-57-1 F: C20H31N3O2S2 W: 409.61
PHT-247 is an inhibitor of the pleckstrin homology (PH) domain of Akt, and it is also an inhibitor of PDPK1 with Kis of
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