|
|
| | GSK 2334470 Basic information |
| Product Name: | GSK 2334470 | | Synonyms: | GSK 2334470;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)-4-pyrimidinyl]-N-cyclohexyl-6-methyl-3-piperidinecarboxamide GSK 2334470;GSK2334470;GSK 2334470;GSK-2334470;((3S,6R)-1-(6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl)-6-methylpiperidin-3-yl)(piperidin-1-yl)methanone;1S,4R)-3-(6-(3-AMINO-1H-INDAZOL-6-YL)-2-(METHYLAMINO)PYRIMIDIN-4-YL)-N-CYCLOHEXYL-4-METHYLCYCLOHEXAN | | CAS: | 1227911-45-6 | | MF: | C25H34N8O | | MW: | 462.59 | | EINECS: | | | Product Categories: | Inhibitors;Akt;mTOR;PI3K;PI3K/Akt/mTOR;API | | Mol File: | 1227911-45-6.mol |  |
| | GSK 2334470 Chemical Properties |
| density | 1.30±0.1 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: ≥10mg/mL | | pka | 12.84±0.40(Predicted) | | form | powder | | 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. |
| | GSK 2334470 Usage And Synthesis |
| 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 |
| | GSK 2334470 Preparation Products And Raw materials |
|