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GSK 2334470

Catalog #: 4143
9 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4143/10
4143/50
GSK 2334470 | CAS No. 1227911-45-6 | PDK-1 Inhibitors
1 Image
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%

Product Details
Citations (9)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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 BrafV600E::Pten(-/-) mice.

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

M.Wt:
462.59
Formula:
C25H34N8O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
1227911-45-6

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.

Additional Information

Licensing Caveats:
Sold for research purposes only under agreement from GlaxoSmithKline

Product Datasheets

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Citations for GSK 2334470

The citations listed below are publications that use Tocris products. Selected citations for GSK 2334470 include:

9 Citations: Showing 1 - 9

  1. Akt phosphorylates insulin receptor substrate to limit PI3K-mediated PIP3 synthesis.
    Authors: Guang Et al.
    Elife  2021;10
  2. Inhibition of class I PI3K enhances chaperone-mediated autophagy.
    Authors: Richard A Et al.
    J Cell Biol  2020;219
  3. The PI3K and MAPK/p38 pathways control stress granule assembly in a hierarchical manner.
    Authors: Heberle Et al.
    Life Sci Alliance  2019;2
  4. The 3-Phosphoinositide-Dependent Protein Kinase 1 Inhibits Rod Photoreceptor Development.
    Authors: Xing Et al.
    Front Cell Dev Biol  2018;6:134
  5. The hVps34-SGK3 pathway alleviates sustained PI3K/Akt inhibition by stimulating mTORC1 and tumour growth.
    Authors: Natalia Et al.
    EMBO J  2016;35:1902-22
  6. Retinoic acid regulates Kit translation during spermatogonial differentiation in the mouse.
    Authors: Busada Et al.
    Oncotarget  2015;397:140
  7. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells.
    Authors: Qi Et al.
    Cancer Cell Int  2015;15:91
  8. Kinome profiling reveals breast cancer heterogeneity and identifies targeted therapeutic opportunities for triple negative breast cancer.
    Authors: Al-Ejeh Et al.
    PLoS One  2014;5:3145
  9. Activation of 3-phosphoinositide-dependent kinase 1 (PDK1) and serum- and glucocorticoid-induced protein kinase 1 (SGK1) by short-chain sphingolipid C4-ceramide rescues the trafficking defect of δF508-cystic fibrosis transmembrane conductance regulat
    Authors: Raymond A Et al.
    J Biol Chem  2014;289:35953-68

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