GSK2334470 | Potent and selective PDK1 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $59.00 | ||
| 25 mg | $245.00 |
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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
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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