For research use only.

Catalog No.S7087

21 publications

GSK2334470 Chemical Structure

CAS No. 1227911-45-6

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.

Selleck's GSK2334470 has been cited by 21 publications

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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.
PDK-1 [1]
(Cell-free assay)
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 cells NHWzbWhHfW6ldHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKFCGS{GtcYVlcWG2ZXSgRWtVKHCqb4PwbI9zgWyjdHnvckBifCCWaIKzNFghemW|aXT1[UBqdiCqdX3hckBRSzNiY3XscJMh[nliRVzJV2EtKEmFNUC9NE4yOTNizszN MlPXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
PC3 cells MUHGeY5kfGmxbjDhd5NigQ>? Mnm5TY5pcWKrdHnvckBw\iCSRFuxMY1m\GmjdHXkJHJUUyCyaH;zdIhwenmuYYTpc44h[XRiU3XyNlIyKHKnc3nkeYUhcW5iaIXtZY4hWEN|IHPlcIx{KGK7IFXMTXNCNCCLQ{WwQVAvOjl|IN88US=> MnfZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
K562 cells MkfwVJJwdGmoZYLheIlwdiCjc4PhfS=> M37SXWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczygTWM2OD1zODFOwG0> NV7JZZEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFE3PzVpPkKxN|QyPjd3PD;hQi=>
OCI-AML2 cells M4HhU3Bzd2yrZnXyZZRqd25iYYPzZZk> M2HtTmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT1PJMWFOVDJiY3XscJMtKEmFNUC9NE4{PSEQvF2= M2PQN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{SxOlc2Lz5{MUO0NVY4PTxxYU6=
OCI-AML3 cells M3fQU3Bzd2yrZnXyZZRqd25iYYPzZZk> NHW4S2FCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;DTU1CVUx|IHPlcIx{NCCLQ{WwQVAvPTJizszN MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN2MU[3OUc,OjF|NEG2O|U9N2F-
F-36P cells MVfQdo9tcW[ncnH0bY9vKGG|c3H5 NVq0WnBbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDGMVM3WCClZXzsd{whUUN3ME2wMlI5KM7:TR?= NYTDZYpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzOFE3PzVpPkKxN|QyPjd3PD;hQi=>
insect cells MnG4SpVv[3Srb36gZZN{[Xl? NWXOOFBtUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBnfWyuIHzlcod1cCCSRFuxJEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKGmwc3XjeEBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFHreEBi[3SrdnH0bY9vKG2nYYP1doVlKG[xcjCzNEBucW6|IHnuJJBz\XOnbnPlJI9nKFupYX3tZVMzWC2DVGDdMEBKSzVyPUCuNFEh|ryP MnfqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN2NEiyOlcoRjJ|NES4NlY4RC:jPh?=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-Myc / Myc / p-p70 / p70 ; 

PubMed: 25762617     

Effect of the PDK1 inhibitor GSK2334470 on MYC and P70 phosphorylation in CNE2/235 cell line by immunoblotting analysis.

pRb / pPDK1 / pAKT / pRSK2 / p70S6K / pPRAS40 / pS6 ; 

PubMed: 28249908     

ER+ MCF-7 and T47D cells were treated for 24 h with DMSO or increasing concentrations of GSK2334470. Lysates were prepared for immunoblot analysis with the indicated antibodies. GSK2334470 treatment diminished the expression of downstream targets of PDK1. 

25762617 28249908
KDM4A / Pol-I ; 

PubMed: 26729372     

U2OScells were serum starved for 24 h. Starved cells were incubated for 30 min with PDK1 inhibitor GSK2334470 (PDK1i), or PI3K inhibitor LY294002 (LY) or DMSO as a control (Untr) and refed with serum in the presence of 5-FUrd and the respective inhibitors (+serum) or left starved (no serum). Thirty minutes after serum addition cells were fixed and analysed by indirect immunofluorescence using antibodies specific to human KDM4A (panels 1) and Pol-I (panels 2); nuclear DNA was stained by DAPI (panels 3). Scale bar, 5 μM. 



Solubility (25°C)

In vitro DMSO 90 mg/mL (194.55 mM)
Ethanol 90 mg/mL (194.55 mM)
Water 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 Information

Molecular Weight 462.59


CAS No. 1227911-45-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1CCC(CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID