ChemicalBook > CAS DataBase List > GSK 2334470

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
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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.
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Safety

WGK Germany 
3
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0217
Product name
GSK2334470
Purity
≥98% (HPLC)
Packaging
5mg
Price
$161
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0217
Product name
GSK2334470
Purity
≥98% (HPLC)
Packaging
25mg
Price
$517
Updated
2024/03/01
Cayman Chemical
Product number
18095
Product name
GSK2334470
Purity
≥98%
Packaging
5mg
Price
$76
Updated
2024/03/01
Cayman Chemical
Product number
18095
Product name
GSK2334470
Purity
≥98%
Packaging
10mg
Price
$142
Updated
2024/03/01
Cayman Chemical
Product number
18095
Product name
GSK2334470
Purity
≥98%
Packaging
25mg
Price
$335
Updated
2024/03/01
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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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GSK 2334470 Suppliers

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1227911-45-6, GSK 2334470Related Search:


  • 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
  • PDK1 inhibitor GS2334470
  • CS-1873
  • GSK 2334470 USP/EP/BP
  • GSK2334470 GSK-2334470
  • 1227911-45-6
  • C25H34N8O
  • Inhibitors
  • Akt
  • mTOR
  • PI3K
  • PI3K/Akt/mTOR
  • API