WYE-125132
| CAS No. | 1144068-46-1 | Cat. No. | BCP02227 |
| Name | WYE-125132 | ||
| Synonyms | WYE 125132;WYE125132; | ||
| Formula | C26H31N7O4 | M. Wt | 519.61 |
| Description | WYE-125132 potently and ATP-competitively inhibits recombinant mTOR kinase with IC50 of 0.19 nM and also shows the high selectivity over various PI3Ks and a panel of 230 protein kinases. [1] In vitro, WYE-125132 exhibits a significant anti-proliferative activity against a panel of tumor cell lines with IC50 ranging from 2 nM (LNCap) to 380 nM (HTC116). Besides, WYE-125132 also causes cell cycle progression, induction of apoptosis, and inhibition of protein synthesis and cell size.WYE-125132 results in a significant reduction in the synthesis of pre-tRNALeu by 72%, 80%, and 53% in actively proliferating cells of MG63, MDA361, and HEK293, respectively by inhibiting mTORC1. Moreover, WYE-125132 is also found to induce the dephosphorylation of Maf1 (negative regulator of Pol III transcription) and its accumulation in the nucleus. | ||
| Pathways | PI3K/Akt/mTOR | ||
| Targets | mTOR | ||
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mTOR Promotes Tissue Factor Expression and Activity in EGFR-Mutant Cancer
Publications Citing of Biochempartner's WYE-125132(CAS:1144068-46-1) |
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mTOR complex-2 stimulates acetyl-CoA and de novo lipogenesis through ATP citrate lyase in HER2/PIK3CA-hyperactive breast cancer
Publications Citing of Biochempartner's WYE-125132(CAS:1144068-46-1) |
Structure
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