| Identification | Back Directory | [Name]
GSK 2334470 | [CAS]
1227911-45-6 | [Synonyms]
CS-1873
GSK 2334470
GSK 2334470 USP/EP/BP
GSK2334470 GSK-2334470
PDK1 inhibitor GS2334470
GSK2334470;GSK 2334470;GSK-2334470
1S,4R)-3-(6-(3-AMINO-1H-INDAZOL-6-YL)-2-(METHYLAMINO)PYRIMIDIN-4-YL)-N-CYCLOHEXYL-4-METHYLCYCLOHEXAN
1S,4R)-3-(6-(3-aMino-1H-indazol-6-yl)-2-(MethylaMino)pyriMidin-4-yl)-N-cyclohexyl-4-MethylcyclohexanecarboxaMide
(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide
3-Piperidinecarboxamide, 1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-, (3S,6R)-
((3S,6R)-1-(6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl)-6-methylpiperidin-3-yl)(piperidin-1-yl)methanone
(3S,6R)-1-[6-(3-Amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide GSK 2334470 | [Molecular Formula]
C25H34N8O | [MDL Number]
MFCD21608525 | [MOL File]
1227911-45-6.mol | [Molecular Weight]
462.59 |
| Chemical Properties | Back Directory | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥10mg/mL | [form ]
powder | [pka]
12.84±0.40(Predicted) | [color ]
white to light brown | [Stability:]
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
GSK2334470 has been used as an inhibitor of 3-phosphoinositide dependent protein kinase-1 (PDK-1) in:
- Treg cells, to identify regulators of interleukin 2 (IL-2)– signal transducer and activator of transcription 5 (STAT5) signaling
- glycodelin-transfected HEC-1B human endometrial adenocarcinoma cells.
- HeLa and Hs578T cells to test its effect on formylglycinamidine ribonucleotide synthase?(FGAMS) assembly
| [Definition]
ChEBI: (3S,6R)-1-[6-(3-amino-1H-indazol-6-yl)-2-(methylamino)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide is a member of indazoles. | [Biochem/physiol Actions]
GSK2334470 (GSK-470) mediates cell cycle arrest. It also inhibits cellular proliferation and induces apoptosis in cancer cells. | [storage]
Store at +4°C | [References]
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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