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GSK2334470

CAS No. : 1227911-45-6

MCE 站：GSK2334470

产品活性：GSK2334470是高效特异性的 PDK1 抑制剂，IC₅₀值为10 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：PDK-1

In Vitro: Small molecule GSK2334470 inhibits PDK1 with an IC₅₀ of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. Addition of GSK2334470 ablates T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1). GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR, respectively, and induce higher G0–G1 ratio in LAN-1-MK than that in LAN-1 as well. PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines.

In Vivo: The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn Braf^V600E::Pten^?/?mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  BX795  |  MP7  |  Polyphyllin I  |  BX-912  |  BX517  |  (R)-PS210  |  PDK1-IN-RS2

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