Art. -Nr.: HY-14981

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GSK2334470

14 Cited Publications

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Based on 14 publication(s) in Google Scholar

GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC₅₀ of 10 nM.

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Reinheit: 99.79%
CAS. Nr.: 1227911-45-6
Formel: C₂₅H₃₄N₈O
Molecular Weight:462.59

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GSK2334470 Chemical Structure

CAS. Nr.: 1227911-45-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC₅₀ of 10 nM.

IC₅₀ & Target

IC50: 10 nM(PDK1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	>30 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human HEL 92.1.7 cells Antiproliferative activity against human HEL 92.1.7 cells	[PMID: 21341675]
K562	IC₅₀	18 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 21341675]
OCI-AML2	IC₅₀	0.35 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human OCI-AML2 cells Antiproliferative activity against human OCI-AML2 cells	[PMID: 21341675]
OCI-AML-3	IC₅₀	0.52 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human OCI-AML3 cells Antiproliferative activity against human OCI-AML3 cells	[PMID: 21341675]
PC-3	IC₅₀	113 nM Compound: (3S,6R)-28d, GSK-2334470	Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA	[PMID: 21341675]
PC-3	IC₅₀	293 nM Compound: (3S,6R)-28d, GSK-2334470	Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA	[PMID: 21341675]

In Vitro

Small molecule GSK2334470 inhibits PDK1 with an IC₅₀ of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. Addition of GSK2334470 ablates T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1). GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR, respectively, and induce higher G0–G1 ratio in LAN-1-MK than that in LAN-1 as well. PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn Braf^V600E::Pten^/mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1227911-45-6
Appearance Solid
Molecular Weight 462.59
Formel C₂₅H₃₄N₈O
Color Light yellow to yellow
SMILES

O=C([C@@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[C@H](C)CC1)NC5CCCCC5
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (14)

All WBFlow CytometryHistological Imaging/StainingCell Proliferation/Viability Assay

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

Discovery, delineation, and therapeutic targeting of a hyper-translation pathway driving cytokine release syndrome. [Abstract]

2025 Dec 30:102531. PMID: 41475340
Br J Cancer

A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity. [Abstract]

2020 Aug;123(4):542-555. PMID: 32439931

GSK2334470 purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2020 Aug;123(4):542-555. [Abstract]

The combination of the PDK1 inhibitor GSK2334470 with AKT inhibitors of either class potentiated cell death in MDA-MB-361 cells
Chin Med

Gynostemma Pentaphyllum ameliorates CCl4-induced liver injury via PDK1/Bcl-2 pathway with comprehensive analysis of network pharmacology and transcriptomics. [Abstract]

2024 May 15;19(1):70. PMID: 38750545

GSK2334470 purchased from MedChemExpress. Usage Cited in: Chin Med. 2024 May 15;19(1):70. [Abstract]

GPE promoted the phosphorylation of PDK1, PI3K, and Akt; however, those effect were abrogated by GSK2334470 (1 μM) treatment.
Neurobiol Dis

Deletion of PDK1 in oligodendrocyte lineage cells causes white matter abnormality and myelination defect in the central nervous system. [Abstract]

2021 Jan;148:105212. PMID: 33276084
iScience

GSK2334470 attenuates high salt-exacerbated rheumatoid arthritis progression by restoring Th17/Treg homeostasis. [Abstract]

2024 Apr 26;27(6):109798. PMID: 38947509

GSK2334470 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Apr 26;27(6):109798. [Abstract]

CD4 T cells from RA patients were isolated and treated with HS and/or GSK2334470 (GSK) (2.5 μM) for 3 days, and the proportion of Th17 cells was detected by flow cytometry.

GSK2334470 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Apr 26;27(6):109798. [Abstract]

GSK2334470 (GSK) (25 mg/kg, i.p.) treatment alleviated these arthritic symptoms and counteracted the adverse effects of HS diet on RA progression.
J Biol Chem

Cellular stress induces non-canonical activation of the receptor tyrosine kinase EphA2 through the p38-MK2-RSK signaling pathway. [Abstract]

2023 May;299(5):104699. PMID: 37059179
Development

Axin1 regulates tooth root development by inhibiting AKT1-mTORC1 activation and Shh translation in Hertwig's epithelial root sheath. [Abstract]

2024 Nov 1;151(21):dev202899. PMID: 39344774
Biol Pharm Bull

Non-canonical Activation of RSK1 Induces EphA2-Mediated Cell Migration under Cellular Stress Conditions. [Abstract]

2025;48(7):1089-1095. PMID: 40721370
bioRxiv

PDK1 and YAP1/TEAD signaling drive acquired KRAS inhibitor resistance in KRAS-mutant non-small cell lung cancer. [Abstract]

2025 Dec 25:2025.12.22.696060. PMID: 41509231
Biomed Pharmacother

Drug target proteome profiling identifies HES1-driven mitotic catastrophe in ovarian serous carcinoma. [Abstract]

2025 Nov 6:193:118716. PMID: 41202420
Universidad de Granada

2020 Sep.
Oncotarget

Concomitant inhibition of receptor tyrosine kinases and downstream AKT synergistically inhibited growth of KRAS/BRAF mutant colorectal cancer cells. [Abstract]

2017 Jan 17;8(3):5003-5015. PMID: 28002807

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (108.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1617 mL

10.8087 mL

21.6174 mL

5 mM

0.4323 mL

2.1617 mL

4.3235 mL

10 mM

0.2162 mL

1.0809 mL

2.1617 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[2]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Mice is dissolved in DMSO and then diluted with PBS or saline. Braf^V600E::Pten^−/− are generated as previously described. Cohorts of six animals per group are used in each experimental group. GSK2334470 is administered through IP injection (100 mg/kg) 3 times per week starting the same day of topical administration of 4-hydroxytamoxifen and ending at the time of mouse collection, based on earlier studies^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Najafov A, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J.?2011 Jan 15;433(2):357-69. [Content Brief]

[2]. Qi L, et al. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int.?2015 Sep 29;15:91. [Content Brief]

[3]. Scortegagna M, et al. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1617 mL	10.8087 mL	21.6174 mL	54.0435 mL
	5 mM	0.4323 mL	2.1617 mL	4.3235 mL	10.8087 mL
	10 mM	0.2162 mL	1.0809 mL	2.1617 mL	5.4044 mL
	15 mM	0.1441 mL	0.7206 mL	1.4412 mL	3.6029 mL
	20 mM	0.1081 mL	0.5404 mL	1.0809 mL	2.7022 mL
	25 mM	0.0865 mL	0.4323 mL	0.8647 mL	2.1617 mL
	30 mM	0.0721 mL	0.3603 mL	0.7206 mL	1.8015 mL
	40 mM	0.0540 mL	0.2702 mL	0.5404 mL	1.3511 mL
	50 mM	0.0432 mL	0.2162 mL	0.4323 mL	1.0809 mL
	60 mM	0.0360 mL	0.1801 mL	0.3603 mL	0.9007 mL
	80 mM	0.0270 mL	0.1351 mL	0.2702 mL	0.6755 mL
	100 mM	0.0216 mL	0.1081 mL	0.2162 mL	0.5404 mL

Keywords

GSK2334470

14 Cited Publications

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GSK2334470

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GSK2334470

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2334470

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Anti-Pancreatic Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Glucose Metabolism Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) GSK2334470

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK2334470 Related Classifications

HY-14981 Related Classifications