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Results for "

pyruvate kinase isoforms

" in MedChemExpress (MCE) Product Catalog:

10

Inhibitors & Agonists

3

Natural
Products

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-126585
    SAICAR
    4 Publications Verification

    		 Endogenous Metabolite Cancer
    SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
    SAICAR
  • HY-121744
    PS10
    Maximum Cited Publications
    6 Publications Verification

    		 PDHK Inflammation/Immunology
    PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
    PS10
  • 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 .
    TM-1
  • HY-112253
    D-Fructose 1-phosphate

    		Endogenous Metabolite Metabolic Disease
    D-Fructose 1-phosphate is a key intermediate metabolite in the fructose metabolic pathway. As a key signaling molecule linking fructose metabolism and glucose metabolic regulation, D-Fructose 1-phosphate acts as an allosteric modulator to counteract the inhibitory effect of the glucokinase-regulatory protein complex, thereby finely regulating the direction of hepatic glucose metabolism at the substrate level .
    D-Fructose 1-phosphate
  • HY-167832
    PT109

    		JNK SGK ROCK Tau Protein MMP DNA/RNA Synthesis Pyruvate Kinase NF-κB COX NO Synthase Reactive Oxygen Species (ROS) Neurological Disease Cancer
    PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease .
    PT109
  • HY-114702
    M77976
    2 Publications Verification

    		 PDHK Metabolic Disease
    M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes .
    M77976
  • HY-N15451
    Deoxytopsentin

    		Pyruvate Kinase Infection
    Deoxytopsentin (compound 5) is a marine bisindole alkaloid and also a MRSA pyruvate kinase inhibitor. Deoxytopsentin exists in sponges. Deoxytopsentin exhibits antibacterial activity against methicillin-resistant Staphylococcus aureus strains in vitro .
    Deoxytopsentin
  • HY-111936
    ML 083

    BML283

    		 Pyruvate Kinase Cancer
    ML083 is a member of a series of highly specific allosteric activators for the tumor-specific isoform of human pyruvate kinase (M2 isoform). ML083 affects the cooperativity of phosphoenolpyruvate (PEP) binding. ML083 can be used in the research of tumors .
    ML 083
  • HY-126585S
    SAICAR-d3

    		Endogenous Metabolite Metabolic Disease
    SAICAR-d3 is the deuterium labeled SAICAR. SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvate kinase isoform M2 (PKM2) in an isozyme-selective manner, with an EC50 of 0.3 mM. SAICAR stimulates PKM2 and promotes cancer cell survival in glucose-limited conditions .
    SAICAR-d3
  • HY-183765
    PARP1/PKM2-IN-1

    		PARP Pyruvate Kinase Cancer
    PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma .
    PARP1/PKM2-IN-1

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