Catalog No.S7087

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.

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GSK2334470 Chemical Structure

GSK2334470 Chemical Structure
Molecular Weight: 462.59

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Quality Control & MSDS

Product Information

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  • Inhibition Profile

Product Description

Biological Activity

Description GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.
Targets PDK-1 [1]
(Cell-free assay)
IC50 10 nM
In vitro GSK2334470 inhibits PDK1 from activating full-length Akt1 in the presence of PtdIns(3,4,5)P3-containing lipid vesicles or a mutant of Akt1 lacking the PH domain (ΔPH-Akt1) with IC50 of ~10 nM. GSK2334470 also similarly inhibits PDK1 from phosphorylating the PDKtide peptide substrate with IC50 of ~10 nM. GSK2334470 (0.1 μM–0.3 μM) induces significant dose-dependent inhibition of endogenous NDRG1 with over 50% reduction in phosphorylation in HEK-293 cells. GSK2334470 (30 nM) induces a significant dose-dependent inhibition of the T-loop phosphorylation of each SGK isoform in HEK-293 cells. GSK2334470 (1 μM) inhibits hydrophobic motif phosphorylation of S6K1 to a similar extent as T-loop phosphorylation in HEK-293 cells. GSK2334470 (3 μM) also suppresses S6K1 activity and phosphorylation induced by IGF1 stimulation of serum-starved HEK-293 cells. GSK2334470 (3 μM) markedly inhibits the phosphorylation of several Akt substrates [FoxO (forkhead box O), GSK3 and PRAS40]. GSK2334470 (3 μM) also induces near maximal inhibition of Akt1 activity and phosphorylation within 5 min, and Akt substrate phosphorylation (FoxO, GSK3 and PRAS40) is inhibited at a slightly later time point (10 min). GSK2334470 (0.3 μM) significantly inhibits phosphorylation of Akt or PRAS40/GSK3 in PDK1K465E/K465E knock-in but not wild-type ES cells. GSK2334470 (1 μM) effectively suppresses SGK1 activity as judged by the inhibition of NDRG1 phosphorylation in U87 glioblastoma cells. GSK2334470 (1 μM) also potently suppresses activation of S6K1 (Figure 7B) as well as SGK1 in MEF (mouse embryonic fibroblast) cells. GSK2334470 (0.1 μM) induces ~50% inhibition of RSK2 activity in HEK-293 cells. [1] GSK2334470 (30 µM) suppresses U46619 induced Ca2+-sensitized force in α-toxin permeabilized rabbit pulmonary artery SM. GSK2334470 (30 µM) results in a significant decrease in the contractile force in response to [Ca2+]. [2] GSK2334470 (1 μM) results in total abrogation of the EGF-induced intracellular calcium increase and inositol phosphates accumulation in MDA-MB-231 cells. GSK2334470 (1 μM) inhibits PLCγ1 Tyr783 phosphorylation in MDA-MB-231 cells. [3]
In vivo

Protocol(Only for Reference)

Kinase Assay: [1]

Kinase activity assays Endogenous Akt, S6K and RSK are immunoprecipitated from 0.1 mg to 1 mg of cell lysate for 2 hours at 4℃ on a vibrating platform using 3 μg–5 μg of the indicated antibodies. For the SGK activity assays, 150 μg of transfected lysate is incubated with 5 μg of glutathione–Sepharose for 3 hours at 4℃. The immunoprecipitates are washed twice with lysis buffer containing 0.5 mM NaCl, followed by two washes with kinase buffer. Kinase reactions are initiated by a reaction mixture to bring the final concentrations of the reaction components to 0.1 mM [γ-32P]ATP (~200 c.p.m./pmol), 5 mM magnesium acetate, 0.1% 2-mercaptoethanol and 30 mM Crosstide peptide (GRPRTSSFAEGKK). Reactions are carried out for 20 min at 30℃ on a vibrating platform and stopped by spotting the reactions on to P81 phosphocellulose paper. Cerenkov counting is done after washing the papers in phosphoric acid, rinsing in acetone and air-drying. One unit of activity is defined as that which catalysed the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 hour.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Najafov A, et al. Biochem J, 2011, 433(2), 357-369.

[2] Artamonov M, et al. PLoS One, 2013, 8(3), e58703.

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Chemical Information

Download GSK2334470 SDF
Molecular Weight (MW) 462.59


CAS No. 1227911-45-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 90 mg/mL (194.55 mM)
Ethanol 90 mg/mL (194.55 mM)
Water <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 3-Piperidinecarboxamide, 1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-, (3S,6R)-

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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