pyruvate dehydrogenase

Nitrofurazone (Nitrofural; Furacilin) is an orally active nitroaromatic broad-spectrum antibiotic with activity against both Gram-positive and Gram-negative bacteria. It is commonly used for establishing breast cancer models.

Pyruvate Kinase/Lactic Dehydrogenase enzymes, Rabbit catalyze the ATP-dependent phosphorylation of glycolate to produce 2-phosphoglycolate. The activation of pyruvate kinase requires divalent cation Mg2+ and monovalent cation K+.

Dehydroabiethylamine (NSC-2955) is an inducer of hepatic CYP2B activity. Dehydroabiethylamine inhibits pyruvate dehydrogenase kinases (PDKs) and intracellular cholesterol transport with anti-tumor activity.

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.

Dicoumarol (Dicumarol) is a hydroxycoumarin originally isolated from molding sweet-clover hay, with anticoagulant and vitamin K depletion activities. Dicoumarol is a competitive inhibitor of vitamin K epoxidereductase; thus, it inhibits vitamin K recycling and causes depletion of active vitamin K in blood. This prevents the formation of the active form of prothrombin and several other coagulant enzymes, and inhibits blood clotting.

KPLH1130, a specific pyruvate dehydrogenase kinase (PDK) inhibitor, enhances glucose tolerance in mice fed a high-fat diet (HFD). It effectively hinders macrophage polarization and mitigates proinflammatory reactions.

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.

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

JX06, a potent, selective and covalent PDK inhibitor, inhibits PDK1, PDK2 and PDK3 with IC50 of 49 nM, 101 nM and 313 nM respectively.

AZD7545 is a potent PDHK inhibitor.

(L)-Sodium lactate (Sodium L-Lactate) is produced from pyruvate by the enzyme Lactate Dehydrogenase. Lactate production occurs during anaerobic glycolysis or in proliferatively active cells. L-Lactic Acid occurs in small quantities in the blood and muscle fluid of man and animals. The lactic acid concentration increases in muscle and blood after vigorous activity. L-Lactic acid is also present in liver, kidney, thymus gland, human amniotic fluid, and other organs and body fluids.

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.

LDHA-IN-8, a small molecule inhibitor of lactate dehydrogenase A (LDHA), inhibits the proliferation of pancreatic and lung cancer cells by inhibiting the activity of LDHA-catalyzed pyruvate in a dose-dependent manner (EC 50=14.54μM), decreasing the intracellular lactate content and increasing the intracellular reactive oxygen species (ROS) levels.

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.

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.

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.

FX-11 (LDHA Inhibitor FX11) is a highly potent, selective, and competitive inhibitor of lactate dehydrogenase A (LDHA), with a Ki value of 8 μM for LDHA. FX-11 acts as an activator of PKM2 (pyruvate kinase M2). FX-11 exerts its antitumor effects by inhibiting glycolysis, depleting ATP, and inducing oxidative stress and apoptosis. FX-11 can be used in tumor metabolism research.

PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 with an IC50 value of 1.5 μM, demonstrating anticancer properties. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), thereby restricting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 leads to increased reliance on glycolysis (Warburg effect). PDHK1-IN-1 inhibits phosphorylation at the PDHK1 recognition site PDC E1α Ser232 and also suppresses phosphorylation of Ser293.

PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinase 1/2 (PDHK1/2), with an IC50 of 0.007 μM for PDHK1 and 0.015 μM for PDHK2. PDHK1-IN-2 has the potential to regulate immune cell metabolism and correct mitochondrial dysfunction, making it a promising candidate for research in autoimmune diseases, inflammatory conditions, and cancer.

JNK-IN-23 (Compound K12) is an inhibitor of JNK. It effectively inhibits the proliferation of MDA-MB-231 cells with a GIC50 of 30 nM. In vivo, JNK-IN-23 blocks metastatic growth of triple-negative breast cancer (TNBC). Additionally, it suppresses the growth of lung metastases by dual targeting of glutaminase-1 (GLS) and the pyruvate dehydrogenase complex (PDHC).

PDHc-E2-IN-1 (Compound 9) is an inhibitor of the pyruvate dehydrogenase complex E2 (PDHc-E2), with an IC50 value of 2.52 μM. It exhibits potent antibacterial activity and can be utilized in research related to bacterial brown stripe and bacterial leaf blight in rice.

Galloflavin is a lactate dehydrogenase inhibitor that inhibits the activity of lactate dehydrogenase. Galloflavin inhibits both human LDH isoforms (type A and type B) by preferentially binding to the free enzyme without competing with substrates or cofactors, with Ki values ​​calculated by pyruvate of 5.46 μM (LDH-A) and 15.06 μM (LDH-B).

Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.

PDHK-IN-3 (compound 7) is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK) with IC50 values of 0.21 μM for PDHK2 and 1.54 μM for PDHK4 [1].