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GSK2334470

Cat. No. M2115
GSK2334470 Structure
Size Price Availability Quantity
10mg USD 90  USD90 In stock
50mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

GSK2334470 is a potent and selective PDK1 (3-Phosphoinositide dependent protein kinase-1) inhibitor. GSK2334470 blocks the phosphorylation of known PDK1 substrates, but surprisingly find that the potency and kinetics of inhibition vary for different PDK1 targets. GSK2334470 subsequent activation of PDK1 substrates S6K1, SGK and RSK in HEK293, U87 and mouse embryonic fibroblast cell lines. GSK2334470 inhibited activation of an Akt1 mutant lacking the PH domain (pleckstrin homology domain) more potently than full-length Akt1, suggesting that GSK2334470 is more effective at inhibiting PDK1 substrates that are activated in the cytosol rather than at the plasma membrane. GSK2334470 also suppressed T-loop phosphorylation and activation of RSK2 (p90 ribosomal S6 kinase 2), another PDK1 target activated by the ERK (extracellular-signal-regulated kinase) pathway.

Customer Product Validations & Biological Datas
Source Oncogene (2014). Figure 2. GSK2334470
Method H&E stain
Cell Lines mice
Concentrations 2.5 μM
Incubation Time 7 days
Results It is noteworthy that while administration of PDKi did not inhibit development of localized melanomas (local application of 4-HT), it reduced metastasis burden in lymph nodes as quantitated by S100 stain
Chemical Information
Molecular Weight 462.59
Formula C25H34N8O
CAS Number 1227911-45-6
Solubility (25°C) DMSO
Ethanol
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Knight ZA. Biochem J. For a PDK1 inhibitor, the substrate matters.

[2] Najafov A, et al. Biochem J. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1.

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Keywords: GSK2334470 supplier, PDK1, inhibitors, activators


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