GSK 2334470

Name: GSK 2334470
Brand: Tocris Bioscience
SKU: 4143

Tocris Bioscience, part of Bio-Techne | Catalog # 4143

Citations (27)

COA / SDS

Highly potent, selective PDPK1 (PDK1) inhibitor

Key Product Details

Description:	Highly potent, selective PDPK1 (PDK1) inhibitor
Chemical Name:	(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	462.59

View Full Technical Details for GSK 2334470

Technical Data
Citations

Biological Activity for GSK 2334470

GSK 2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDPK1) inhibitor (IC₅₀ ~ 10 nM). Exhibits no effect on other kinases including Aurora, ROCK, p38 MAPK and PI 3-K. Suppresses T-loop phosphorylation and subsequent activation of PDK1 substrates S6K1, SGK and RSK in vitro; exhibits limited inhibitory effect on Akt activation. Delays melanomagenesis and metastasis in Braf^V600E::Pten^(-/-) mice.

Licensing Information

Sold for research purposes only under agreement from GlaxoSmithKline

Compound Libraries for GSK 2334470

GSK 2334470 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

External Portal Information

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of GSK 2334470 is reviewed on the chemical probes website.

Technical Data for GSK 2334470

M. Wt	462.59
Formula	C₂₅H₃₄N₈O
Storage	Store at +4°C
Purity	≥98% (HPLC)
CAS Number	1227911-45-6
PubChem ID	46215815
InChi Key	QLPHOXTXAKOFMU-WBVHZDCISA-N
Smiles	C[C@H]1N(C3=NC(NC)=NC(C4=CC(NN=C5N)=C5C=C4)=C3)C[C@@H]([C@](NC2CCCCC2)=O)CC1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for GSK 2334470

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	46.26	100
	ethanol	46.26	100

Preparing Stock Solutions for GSK 2334470

The following data is based on the product molecular weight 462.59.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.16 mL	10.81 mL	21.62 mL
5 mM	0.43 mL	2.16 mL	4.32 mL
10 mM	0.22 mL	1.08 mL	2.16 mL
50 mM	0.04 mL	0.22 mL	0.43 mL

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References for GSK 2334470

References are publications that support the biological activity of the product.

Scortegagna Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf^V600E::Pten^(-/-) melanoma. Oncogene 2014 PMID: 24037523
Najafov Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem.J. 2011 PMID: 21087210