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PKM2 activator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AIM2 (2) Apoptosis (3) Autophagy (1) Caspase (1) Chloride Channel (2) DNA Methyltransferase (2) Endogenous Metabolite (2) Exosomes (2) HIV (2) JAK (1) NF-κB (2) PDK-1 (1) Pyruvate Kinase (17) Reactive Oxygen Species (ROS) (2) Reference Standards (1) STAT (1) TNF Receptor (2)
By Research Areas:	Cancer (17) Inflammation/Immunology (1) Metabolic Disease (2) Neurological Disease (1)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-18657

TEPP-46 50+ Cited Publications ML-265	Pyruvate Kinase	Cancer
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 .

HY-N0822

Shikonin 65+ Cited Publications C.I. 75535; Isoarnebin 4	Exosomes Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2	Cancer
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .

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 .

HY-19330

DASA-58 15+ Cited Publications	Pyruvate Kinase	Metabolic Disease Cancer
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 .

HY-147368

PKM2 activator 2	Pyruvate Kinase	Cancer
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 .

HY-148324

PKM2 activator 5	Pyruvate Kinase	Cancer
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 .

HY-162080

METTL1-WDR4-IN-1 1 Publications Verification	DNA Methyltransferase Pyruvate Kinase	Cancer
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 .

HY-139667

PKM2-IN-3 1 Publications Verification	Pyruvate Kinase	Neurological Disease
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 .

HY-155216

PKM2 activator 10	Pyruvate Kinase	Cancer
PKM2 activator 10 (Compd I) is a *PKM2* activator with anti-tumor activity. PKM2 activator 10 can be utilized in cancer research .

HY-148313

PKM2 activator 4	Pyruvate Kinase	Cancer
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 .

HY-147397

PKM2 activator 3	Pyruvate Kinase	Cancer
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.)

HY-156375

PKM2 activator 6	Pyruvate Kinase PDK-1	Cancer
PKM2 activator 6 (Compound Z10) is a *PKM2* activator and PDK1 inhibitor (K_D: 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) .

HY-161519

PKM2 activator 7	Pyruvate Kinase	Inflammation/Immunology
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 .

HY-132215

PF-06284674 PKM2 activator 1	Pyruvate Kinase	Cancer
PF-06284674 (PKM2 activator 1) (Compound 8) is a *PKM2* activator that can be used in cancer research .

HY-N0822R

Shikonin (Standard) C.I. 75535 (Standard); Isoarnebin 4 (Standard)	Reference Standards Exosomes Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2	Cancer
Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .

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 .

HY-180795

PKM2 activator 11	Pyruvate Kinase STAT Apoptosis	Cancer
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 .

HY-162080A

METTL1-WDR4-IN-1 TFA 1 Publications Verification	DNA Methyltransferase Pyruvate Kinase	Cancer
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 .

HY-155785

MTP	Apoptosis Autophagy Reactive Oxygen Species (ROS) JAK	Cancer
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 .

HY-180523

PKM2-IN-13	Pyruvate Kinase Apoptosis Reactive Oxygen Species (ROS) Caspase	Cancer
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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0822

Shikonin 65+ Cited Publications C.I. 75535; Isoarnebin 4	Quinones Structural Classification Classification of Application Fields Plants Lithospermum erythrorhizon Sieb. et Zucc. Naphthalene Quinones Boraginaceae Disease Research Fields Cancer	Exosomes Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .

HY-126585

SAICAR 4 Publications Verification	Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Ketones, Aldehydes, Acids Disease markers Endocrine diseases Nervous System Disorder Endogenous metabolite Disease Research Fields Source Classification Cancer	Endogenous Metabolite
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 .

HY-N0822R

Shikonin (Standard) C.I. 75535 (Standard); Isoarnebin 4 (Standard)	Quinones Structural Classification Plants Lithospermum erythrorhizon Sieb. et Zucc. Naphthalene Quinones Boraginaceae	Reference Standards Exosomes Chloride Channel Pyruvate Kinase NF-κB TNF Receptor HIV AIM2
Shikonin (Standard) is the analytical standard of Shikonin. This product is intended for research and analytical applications. Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC₅₀ of 6.5 μM . Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .

Cat. No.	Product Name	Chemical Structure

HY-126585S

SAICAR-d3
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 .

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PKM2 activator

Inhibitors & Agonists

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Isotope-Labeled Compounds

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