pdk4

PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

PDK4-IN-1, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM.

M77976 is a selective ATP-competitive inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an inhibitory effect on PDK4, having an IC50 value of 648 μM. It is used for research related to obesity and diabetes.

PS10 is a broad-spectrum PDK inhibitor that inhibits PDK2, PDK4, PDK1, and PDK3. It significantly increases pyruvate dehydrogenase complex activity, and is used in research on obesity and type 2 diabetes.

VER-246608 is an effective and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (IC50s: 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively).VER-246608 disrupts Warburg metabolism and induces context-dependent cytosta

PDK4-IN-2 (compound 8), a pyruvate dehydrogenase kinase 4 (PDK4) inhibitor, exhibits an inhibition concentration (IC 50) of 46 µM. By regulating bioenergetics and activating the tricarboxylic acid cycle [1], it enhances the ejection fraction in failing hearts.

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

GSK-7227, a novel compound representing a novel class of peroxisome proliferator-activated receptor delta (PPARδ) partial agonists, demonstrates potent partial agonistic activity by upregulating the expression of PPARδ target genes, specifically carnitine palmitoyltransferase 1a (CPT1a) and pyruvate dehydrogenase kinase 4 (PDK4), in cultured skeletal muscle cells, indicating its potential role in modulating skeletal muscle metabolism and energy homeostasis.

DHNA (KIS20) is an inhibitor of PDH kinase 4 (PDK4) with an IC50 of 18 μM, and is utilized in heart failure research.

PDK-IN-2 (Compound 1F), with an IC50 of 68 nM, is a potent PDK inhibitor that downregulates the expression of PDK1 and PDK4 in cells. It promotes mitochondrial bioenergetics, reduces glycolytic activity, and triggers apoptosis via the mitochondrial pathway. Additionally, PDK-IN-2 has been shown to impede tumor growth in a 4T1 syngeneic mouse model [1].