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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 "
PKM2 activator
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "PKM2 activator" in MCE Product Catalog:
72
72 Publications Verification
Synonyms: C.I. 75535; Isoarnebin 4
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TEPP-46 (ML-265) is a potent and selective pyruvate kinase M2 (PKM2) activator with an AC50 of 92 nM, showing little or no effect on PKM1, PKL and PKR .
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18 Cited Publications
Cat. No.: HY-19330
CAS No.: 1203494-49-8
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DASA-58 is a potential pyruvate kinase isozyme (PKM2) allosteric activator. DASA-58 can be used for the research of metabolism and kinds of cancer .
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Category:
Human Gut Microbiota Metabolites Microorganisms Ketones, Aldehydes, Acids Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Disease Research Fields Cancer
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2
2 Cited Publications
Cat. No.: HY-162080
CAS No.: 374705-10-9
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METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
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2 Cited Publications
Cat. No.: HY-162080A
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METTL1-WDR4-IN-1 (Compound 1) TFA is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50=144 μM). METTL1-WDR4-IN-1 TFA inhibits the m 7G methyltransferase activity of the METTL1-WDR4 complex, blocking the m 7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 TFA can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8 + T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 TFA can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy .
1
1 Cited Publications
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PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation .
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PKM2 activator 2 (compound 28) is a pyruvate kinase M2 (PKM2) activitor with an AC50 value of 66 nM. PKM2 activator 2 can restore normal glycolytic metabolism in cells .
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PKM2 activator 5 (compound 8) is a PKM2 activator with an AC50 value of 0.316 µM. PKM2 activator 5 has the potential to alter the aberrant metabolism of cancer cells .
Cat. No.: HY-155216
CAS No.: 2490276-04-3
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PKM2 activator 10 (Compd I) is a PKM2 activator with anti-tumor activity. PKM2 activator 10 can be utilized in cancer research .
Cat. No.: HY-148313
CAS No.: 781656-66-4
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PKM2 activator 4 is a PKM2 activator with an AC50 value of 1-10 μM. PKM2 activator 4 can be used for the research of cancer .
Cat. No.: HY-147397
CAS No.: 1346113-84-5
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PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
(AC50: the concentration which gives 50% activation of enzyme.)
(AC50: the concentration which gives 50% activation of enzyme.)
Cat. No.: HY-156375
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PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
Cat. No.: HY-161519
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PKM2 activator 7 (Compd B4) is a PKM2 activator with the AC50 of 0.144 μM. PKM2 activator 7 suppresses DSS (HY-116282C)-induced colitis by inhibiting T cell growth in mouse colitis model .
Cat. No.: HY-132215
CAS No.: 1434288-24-0
Synonyms: PKM2 activator 1
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PF-06284674 (PKM2 activator 1) (Compound 8) is a PKM2 activator that can be used in cancer research .
Cat. No.: HY-126585S
Cat. No.: HY-180795
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PKM2 activator 11 (Compound 23) is a PKM2 activator with an AC50 value of 92.12 nM. PKM2 activator 11 promotes PKM2 tetramerization and inhibits its nuclear translocation. PKM2 activator 11 suppresses glycolysis and the PKM2/STAT3 signaling pathway. PKM2 activator 11 induces Apoptosis. PKM2 activator 11 exhibits anti-CRC activity in vitro with potency and selectivity .
Cat. No.: HY-155785
CAS No.: 2377372-62-6
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MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
Cat. No.: HY-180523
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PKM2-IN-13 is a selective PKM2 inhibitor inhibiting PKM2 with an IC50 value of 55.13 μM. PKM2-IN-13 exhibits broad-spectrum anticancer activity with low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevated ROS levels and activation of caspases 3/7, and interacts with and inhibits the glycolytic activity of Pyruvate Kinase M2 in virto. PKM2-IN-13 demonstrates a favorable safety profile with no significant adverse effects in vivo. PKM2-IN-13 can be used for oral squamous cell carcinoma (OSCC), colon carcinoma, breast cancer and melanoma research .
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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
