PDHK1-IN-1
PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 (IC50=1.5 μM) with anticancer activity. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), limiting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 can shift the metabolism towards an increased glycolysis dependence (Warburg effect) . PDHK1-IN-1 can inhibit the phosphorylation of the PDC E1α Ser232 recognition site of PDHK1 and the phosphorylation of Ser293[1].
Product Specifications
UNSPSC
12352005
Target
PDHK
Related Pathways
Metabolic Enzyme/Protease
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
ClC1=CC=C(C(S(=O)(NC2=C(C=CC(C(O)=O)=C2)Br)=O)=C1)C
Molecular Formula
C14H11BrClNO4S
Molecular Weight
404.66
References & Citations
[1]Baber MA, et al. Identification of a selective pyruvate dehydrogenase kinase 1 (PDHK1) chemical probe by virtual screening. Eur J Med Chem. 2025 Feb 15;284:117210.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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