PDK1-IN-6
PDK1-IN-6 is a PDK1 inhibitor (IC50 = 0.06 μM) and also inhibits PDK4 catalytic activity. PDK1-IN-6 inhibits HSP90 ATPase activity. PDK1-IN-6 reduces intracellular lactate accumulation, dissipates mitochondrial membrane potential, and induces Apoptotic cell death. PDK1-IN-6 shifts metabolism from glycolysis to oxidative phosphorylation and increases cellular oxygen consumption. PDK1-IN-6 exhibits anticancer activity against pancreatic cancer.
For research use only. We do not sell to patients.
- Formula: C19H18N6O2
- Molecular Weight:362.39
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HSP90 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PSN1 | IC50 |
70.8 μM
|
Cytotoxicity against human PSN-1 pancreatic ductal adenocarcinoma cells assessed as viability reduction incubated 72 hrs by MTT assay.
Cytotoxicity against human PSN-1 pancreatic ductal adenocarcinoma cells assessed as viability reduction incubated 72 hrs by MTT assay.
|
42574799 |
| PSN1 | IC50 |
57.8 μM
|
Cytotoxicity against human PSN-1 pancreatic cancer 3D spheroids assessed as viability reduction incubated 72 hrs by modified acid phosphatase assay.
Cytotoxicity against human PSN-1 pancreatic cancer 3D spheroids assessed as viability reduction incubated 72 hrs by modified acid phosphatase assay.
|
42574799 |
In Vitro
PDK1-IN-6 (30 min at room temperature) inhibits recombinant PDK1 with an IC50 of 0.06 μM[1].
PDK1-IN-6 (1.5 μM; 30 min at 37 °C and 30 min at 4 °C) completely eliminates HSP90 ATPase activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PSN-1 pancreatic cancer cells
-
Concentration:IC50 concentration
-
Incubation Time:24 h
-
Result:Markedly reduced phosphorylation of Ser232 on PDHA1.
-
Cell Line:PSN-1 pancreatic cancer cells
-
Concentration:IC50 concentration
-
Incubation Time:48 h
-
Result:PSN-1 cells displayed intense nuclear fluorescence, chromatin condensation, and nuclear fragmentation, in contrast to uniformly stained control nuclei.
- Kinase activity and phosphorylation assays
- Western Blot
- Mitochondrial membrane-potential fluorescent assay
- Detection of Apoptosis
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
Chemical Information
-
Molecular Weight 362.39
-
Formula C19H18N6O2
-
SMILES
NC1=NC(C2=CN(C)C3=C2C=C(OC)C=C3)=C(C4=CC=C(OC)N=C4)N=N1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDK1-IN-6 Related Classifications
HY-190664 Related Classifications
Powered by Bioz