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GSK2334470 | Potent and selective PDK1 inhibitor

GSK2334470 (1227911-45-6) is a potent (IC50 = 10 nM) and selective inhibitor of 3-Phosphoinositide-dependent kinase 1 (PDK1), which phosphorylates and activates a group of protein kinases in the AGC/PKG/PKC family.1 It is more effective at inhibiting PDK1 substrates that are activated in the cytosol rather than at the plasma membrane.1 GSK2334470 delayed melanogenesis and metastasis in Braf(V600E)::Pten(-/-) mice.2 It also displays antitumor activity against multiple myeloma synergistically with mTORC1/2 inhibitor PP2423 and proteasome inhibitor MG-1324.

References/Citations
1) Najafov et al. (2011), Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1; Biochem.J. 433 37
2) Scortegagna et al. (2014), Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf (V600E)::Pten(-/-) melanoma; Oncogene 33 4330
3) Yang et al. (2017),PDK1 inhibitor GSK2334470 exerts antitumor activity in multiple myeloma and forms a novel multitargeted combination with dual mTORC1/C2 inhibitor PP242; Oncotarget 8 39185
4) Zhang et al. (2018), PDK1 inhibitor GSK2334470 synergizes with proteasome inhibitor MG-132 in multiple myeloma cells by inhibiting full AKT activity and increasing nuclear accumulation of PTEN protein; Oncol.Rep. 39 2951

 

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Catalog#  10-4725-0005

$59.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
1227911-45-6
Catalog Number:
10-4725
Activity:
Potent and selective PDK1 inhibitor
Chemical Name:
(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
Molecular Weight:
462.60
Molecular Formula:
C25H34N8O
Solubility:
Soluble in DMSO (> 25 mg/ml).
Physical Properties:
Off-white solid
Purity:
>98% by HPLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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