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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
20 Results for "
PDHK
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "PDHK" in MCE Product Catalog:
4
4 Cited Publications
Cat. No.: HY-16082
CAS No.: 252017-04-2
Target:
Research Areas:
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 .
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 .
Cat. No.: HY-146552
CAS No.: 3065641-69-9
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PDHK-IN-4 (Compound 30) is a potent inhibitor of PDHK with IC50s of 0.0051 and 0.0122 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-4 has the potential for the research of cancer diseases .
Cat. No.: HY-173301
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PDHK1-IN-3 (Compound 29) is a selective PDHK1 inhibitor with an IC50 of 0.028 μM against PDHK1 and an IC50 of 0.120 μM against PDHK2. PDHK1-IN-3 inhibits the activity of PDHK1 by forming a covalent bond with Lys299 in PDHK1. PDHK1-IN-3 can be used in the research of autoimmune diseases, inflammatory diseases, and cancer .
Cat. No.: HY-173298
CAS No.: 2870691-38-4
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PDHK1-IN-2 (Compound 24) is an ATP-competitive dual inhibitor of pyruvate dehydrogenase kinases 1/2 (PDHK1/2), with an IC50 of 0.007 μM for PDHK1 and an IC50 of 0.015 μM for PDHK2. PDHK1-IN-2 can regulate immune cell metabolism and correct mitochondrial dysfunction, and is expected to be used in the research of autoimmune diseases, inflammatory diseases, cancers, and other conditions .
Cat. No.: HY-170838
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 .
Cat. No.: HY-146554
PDHK-IN-5 (Compound 19) is a potent inhibitor of PDHK with IC50s of 0.006 and 0.0329 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating agent targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases .
Cat. No.: HY-176008
CAS No.: 2095306-47-9
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Lauric acid leelamide is the lauric acid (C-12) amide analog of Leelamine (HY-W005629). Leelamine exhibits inhibitory activity against pyruvate dehydrogenase kinase (PDHK) with an IC50 value of 9.5 µM. Leelamine derivatives possess anti-inflammatory effects and can inhibit phospholipase A2 activity from various sources .
Cat. No.: HY-L058
1,341 compounds
Glycolysis is a series of metabolic processes by which one molecule of glucose is catabolized to two molecules of pyruvate with a net gain of two ATP. Glycolysis takes place in 10 steps and catalyzed by a series of enzyme, such as hexokinase, Glucose-6-phosphate isomerase, Phosphofructokinase, etc. Glycolysis is used by all cells in the body for energy generation.
Most cancer cells exhibit increased glycolysis and use this metabolic pathway for generation of ATP as a main source of their energy supply. This phenomenon is known as the Warburg effect and is considered as one of the most fundamental metabolic alterations during malignant transformation. Because increased aerobic glycolysis is commonly seen in a wide spectrum of human cancers, development of novel glycolytic inhibitors as a new class of anticancer agents is likely to have broad therapeutic applications.
MCE provides a unique collection of 1,341 glycolysis compounds that mainly target hexokinase, glucokinase, enolase, pyruvate kinase, PDHK, etc. MCE Glycolysis Compound Library is a useful tool for glucose metabolism research and anti-cancer drug discovery.
Cat. No.: HY-P703578
Purity: ≥ 85%, as determined by reducing SDS-PAGE.
Synonyms: PDHK3
Species:
Source:
Cat. No.: HY-P74639
Purity: ≥ 80%, as determined by reducing SDS-PAGE.
Synonyms: Pyruvate dehydrogenase kinase isoform 4; PDK4; PDHK4
Species:
Source:
Cat. No.: HY-P705854
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: PDHK2; Pyruvate dehydrogenase kinase isoform 2 (PDH kinase 2; PDKII)
Species:
Source:
Cat. No.: HY-P705581
Synonyms: Pyruvate dehydrogenase kinase isoform 1; PDH kinase 1 ; PDHK1; EC:2.7.11.2
Species:
Source:
Cat. No.: HY-P706083
Purity: ≥ 80%, as determined by reducing SDS-PAGE.
Synonyms: [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial; Pyruvate dehydrogenase kinase isoform 1; PDH kinase 1; PDHK1
Species:
Source:
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
