1227911-45-6
GSK2334470
CAS: 1227911-45-6
Molecular Formula: C25H34N8O
1227911-45-6 - Names and Identifiers
1227911-45-6 - Physico-chemical Properties
| Molecular Formula | C25H34N8O |
| Molar Mass | 462.59 |
| Density | 1.30±0.1 g/cm3(Predicted) |
| Solubility | DMSO: ≥10mg/mL |
| Appearance | Morphological powder |
| Color | white to light brown |
| pKa | 12.84±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| MDL | MFCD21608525 |
| Physical and Chemical Properties | Bioactive GSK2334470 is a new, highly specific PDK1 inhibitor with an IC50 of about 10 nM and is inactive against other AGC-kinase-closely related proteins. |
| Use | GSK2334470 |
1227911-45-6 - Risk and Safety
| WGK Germany | 3 |
1227911-45-6 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.162 ml | 10.809 ml | 21.617 ml |
| 5 mM | 0.432 ml | 2.162 ml | 4.323 ml |
| 10 mM | 0.216 ml | 1.081 ml | 2.162 ml |
| 5 mM | 0.043 ml | 0.216 ml | 0.432 ml |
Last Update：2024-01-02 23:10:35
1227911-45-6 - Uses and synthesis methods
in vitro studies
In the presence of lipid vesicles containing PtdIns(3,4,5)P3 or Akt1 mutants lacking PH domain (& Delta;PH-Akt1), GSK2334470 inhibits PDK1 by activating full-length Akt1, IC50 is 10 nM. GSK2334470 also inhibits PDK1 by phosphorylation of PDKtide polypeptide substrate, with IC50 of 10 nM. GSK2334470(0.1 μM-0.3 μM) acts on HEK-293 cells to significantly inhibit endogenous NDRG1 and reduce phosphorylation by more than 50%. This effect is dose-dependent. GSK2334470 (30 nM) acts on HEK-293 cells to significantly inhibit T-loop phosphorylation of each SGK subtype, which is dose-dependent. GSK2334470 (1 μM) acts on HEK-293 cells and inhibits the phosphorylation of the hydrophobic motif of S6K1 to a similar degree as the phosphorylation of the T-loop. GSK2334470(3 μM) acts on serum-starved HEK-293 cells and also inhibits S6K1 activity and phosphorylation induced by IGF1 stimulation. GSK2334470(3 μM) significantly inhibited phosphorylation of some Akt substrates [FoxO (Forkhead Box O), GSK3 and PRAS40]. GSK2334470(3 μM) also inhibited Akt1 activity and phosphorylation to the greatest extent within 5 minutes, and inhibited the phosphorylation of Akt substrates (FOXO,GSK3 and PRAS40) at a later time point (10 minutes). GSK2334470(0.3 μM) acts on PDK1K465E/K465E knockout instead of wild-type ES cells, significantly inhibiting Akt or PRAS40/GSK3 phosphorylation. GSK2334470(1 μM) acts on U87 malignant glioma cells and effectively inhibits SGK1 activity by inhibiting NDRG1 phosphorylation. GSK2334470(1 μM) acts on mouse embryonic fibroblasts (MEF) cells and effectively inhibits S6K1 and SGK1 activation. GSK2334470 (0.1 μM) acts on HEK-293 cells and inhibits 50% RSK2 activity. GSK2334470(30 & micro;M) acts on rabbit pulmonary artery SM permeated by α-toxin, inhibiting the Ca2 + sensitive force induced by U46619. GSK2334470 (30 & micro;M) significantly reduced the contraction force in response to [Ca2 +]. GSK2334470(1 μM) acted on MDA-MB-231 cells and completely abolished EGF-induced intracellular calcium increase and phosphoinositide accumulation. GSK2334470(1 μM) acts on MDA-MB-231 cells and inhibits PLC & gamma;1 phosphorylation at Tyr783 site.
Target
IC50: 10 nM(PDK1)
In vivo studies
The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn Braf V600E ::Pten −/− mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1 .
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: GSK2334470 Visit Supplier Webpage Request for quotationCAS: 1227911-45-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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