GSK2334470

Catalog No.S7087

For research use only.

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.

GSK2334470 Chemical Structure

CAS No. 1227911-45-6

Selleck's GSK2334470 has been cited by 23 publications

Purity & Quality Control

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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.
Targets
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 MUDGeY5kfGmxbjDhd5NigQ>? NEDXXpFKdmirYnn0bY9vKG:oIGDET|EudWWmaXH0[YQhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDDUbJI{ODhicnXzbYR2\SCrbjDoeY1idiCSQ{OgZ4VtdHNiYomgSWxKW0FuIFnDOVA:OC5zMUOg{txO NF;YXnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0NVY4PSd-MkGzOFE3PzV:L3G+
PC3 cells NHPmTYZHfW6ldHnvckBie3OjeR?= NXjvdnpCUW6qaXLpeIlwdiCxZjDQSGsyNW2nZHnheIVlKFKVSzDwbI9{eGixconsZZRqd25iYYSgV4VzOjJzIILld4llfWViaX6gbJVu[W5iUFOzJINmdGy|IHL5JGVNUVODLDDJR|UxRTBwMkmzJO69VQ>? M3fWblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{SxOlc2Lz5{MUO0NVY4PTxxYU6=
K562 cells MlnRVJJwdGmoZYLheIlwdiCjc4PhfS=> MlPoRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|LDDJR|UxRTF6IN88US=> M{fTeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{SxOlc2Lz5{MUO0NVY4PTxxYU6=
OCI-AML2 cells Mnj5VJJwdGmoZYLheIlwdiCjc4PhfS=> NXXBSGxESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPR2kuSU2OMjDj[YxteyxiSVO1NF0xNjN3IN88US=> Mo\qQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
OCI-AML3 cells NUT4SHE1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MlnrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRQ1mtRW1NOyClZXzsd{whUUN3ME2wMlUzKM7:TR?= NHTtXYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO0NVY4PSd-MkGzOFE3PzV:L3G+
F-36P cells M36wZXBzd2yrZnXyZZRqd25iYYPzZZk> M3vPcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iRj2zOnAh[2WubIOsJGlEPTB;MD6yPEDPxE1? MnXuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|NEG2O|UoRjJzM{SxOlc2RC:jPh?=
insect cells NGDaUopHfW6ldHnvckBie3OjeR?= NGWxTldKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKFCGS{GgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hcW6|ZXP0JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQXv0JIFkfGm4YYTpc44hdWWjc4Xy[YQh\m:{IEOwJI1qdnNiaX6gdJJme2WwY3Wgc4YhY2ejbX3hN|JRNUGWUG2sJGlEPTB;MD6wNUDPxE1? NWfsW|VzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO0OFgzPjdpPkKzOFQ5OjZ5PD;hQi=>
Assay
Methods Test Index PMID
Western blot pRb / pPDK1 / pAKT / pRSK2 / p70S6K / pPRAS40 / pS6 ; p-Myc / Myc / p-p70 / p70 28249908 25762617
Immunofluorescence KDM4A / Pol-I 26729372

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 462.59
Formula

C25H34N8O

CAS No. 1227911-45-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCC(CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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