GSK 2334470
- Product Name
- GSK 2334470
- CAS No.
- 1227911-45-6
- Chemical Name
- GSK 2334470
- 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;((3S,6R)-1-(6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl)-6-methylpiperidin-3-yl)(piperidin-1-yl)methanone
- CBNumber
- CB62596521
- Molecular Formula
- C25H34N8O
- Formula Weight
- 462.59
- MOL File
- 1227911-45-6.mol
GSK 2334470 Property
- 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.
Safety
- WGK Germany
- 3
N-Bromosuccinimide Price
- Product number
- SML0217
- Product name
- GSK2334470
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $161
- Updated
- 2024/03/01
- Product number
- SML0217
- Product name
- GSK2334470
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $517
- Updated
- 2024/03/01
- Product number
- 18095
- Product name
- GSK2334470
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $76
- Updated
- 2024/03/01
- Product number
- 18095
- Product name
- GSK2334470
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $142
- Updated
- 2024/03/01
- Product number
- 18095
- Product name
- GSK2334470
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $335
- Updated
- 2024/03/01
GSK 2334470 Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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