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Results for "

PDHK1

" in MedChemExpress (MCE) Product Catalog:

4

Inhibitors & Agonists

1

Recombinant Proteins

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-136882
    TM-1

    		PDHK Cancer
    TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation [1].
    TM-1
  • HY-16082
    AZD7545
    2 Publications Verification

    		 PDHK Metabolic Disease
    AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively [1].
    AZD7545
  • HY-15154
    NG 52
    5+ Cited Publications

    Compound 52

    		 CDK Cancer
    NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p [1] .
    NG 52
  • HY-170838
    PDHK1-IN-1

    		PDHK Cancer
    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].
    PDHK1-IN-1

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