Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H34N8O |
| Molecular Weight | 462.5905 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CNC1=NC(=CC(=N1)N2C[C@H](CC[C@H]2C)C(=O)NC3CCCCC3)C4=CC5=C(C=C4)C(N)=NN5
InChI
InChIKey=QLPHOXTXAKOFMU-WBVHZDCISA-N
InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1
| Molecular Formula | C25H34N8O |
| Molecular Weight | 462.5905 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/21087210 | https://www.ncbi.nlm.nih.gov/pubmed/21175429Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24037523
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21087210 | https://www.ncbi.nlm.nih.gov/pubmed/21175429
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/24037523
GSK2334470 is a highly specific inhibitor of 3-phosphoinositide-dependent protein kinase 1(PDK1). GSK2334470 inhibits PDK1 with an IC₅₀ of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. GSK2334470 has being shown to effectively delay melanomagenesis and metastasis in Braf(V600E):Pten(-/-) mice.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. | 2011 Jan 15 |
|
| For a PDK1 inhibitor, the substrate matters. | 2011 Jan 15 |
|
| Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. | 2014 Aug 21 |
Patents
Sample Use Guides
Mice: GSK224470 was administered through IP injection (100 mg/kg) 3 times per week
Route of Administration:
Intraperitoneal
GSK2334470 (0.1 uM–0.3 uM) induces significant dose-dependent inhibition of endogenous NDRG1 with over 50% reduction in phosphorylation in HEK-293 cells. GSK2334470 (30 nM) induces a significant dose-dependent inhibition of the T-loop phosphorylation of each SGK isoform in HEK-293 cells.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:08:11 GMT 2023
by
admin
on
Sat Dec 16 10:08:11 GMT 2023
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| Record UNII |
QB5BF4GJ87
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| Record Status |
Validated (UNII)
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| Record Version |
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1227911-45-6
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