GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 10 mg | In stock | $ 125 | |
| 50 mg | In stock | $ 416 | |
| 100 mg | In stock | $ 704 |
| Description | GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM. |
| 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 BrafV600E::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. |
| CAS No. | 1227911-45-6 |
| Chemical Formula | C25H34N8O |
| Molecular Weight | 462.59 |
| Solubility | DMSO: ≥ 50 mg/mL (108.09 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
In vivo Formulation Calculator (Clear solution)Calculatorbottom
