| Name | GSK2334470 |
| Description | GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases. |
| Cell Research | GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2]. |
| Kinase Assay | FGFR1-4 Biochemical Assays: FGFR kinase inhibition assays are performed at KM for ATP. Picomolar to low nanomolar concentrations of FGFR proteins are incubated in 1× Kinase Reaction Buffer (KRB) with 1 μM of CSKtide and 50 to 250 of μM ATP at 25°C for 90 minutes in the presence or absence of a dosed concentration series of inhibitor. All reactions are terminated by the addition of Stop buffer, and plates are read on a Caliper EZReader2. IC50 values are fit with a four-parameter log[Inhibitor] versus response model with floating Hill Slope. |
| In vivo | The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 was assessed in newborn BrafV600E::Pten?/? mice through systemic administration of 4-HT. Administering PDK1 twice weekly significantly inhibited pigmented lesions and concurrent melanomagenesis, alongside a notable reduction (~80%) in lung metastases and lymph node metastases, as quantified by H&E staining and S100 immunostaining, respectively. This outcome mirrors the effects observed with the genetic deletion of Pdk1[4]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.13 mM), Sonication is recommended.
Ethanol : 83 mg/mL (179.42 mM), Sonication is recommended.
DMSO : 150 mg/mL (324.26 mM), Sonication is recommended.
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| Keywords | PDK-1 | PDK1 | Inhibitor | inhibit | GSK-2334470 | GSK2334470 | GSK 2334470 |
| Inhibitors Related | Rabusertib | MP7 | M77976 | Sodium dichloroacetate | RS1-PDK1 inhibitor | GSK-7227 | BX795 | Hordenine hydrochloride | Dehydroabiethylamine | Dicoumarol | Osu03012 | PS423 |
| Related Compound Libraries | Highly Selective Inhibitor Library | PI3K-AKT-mTOR Compound Library | Anti-Lung Cancer Compound Library | Glycometabolism Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Kinase Inhibitor Library | Angiogenesis related Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
