2. Search Result
Search Result
Results for "

PKM2+inhibitor

" in MedChemExpress (MCE) Product Catalog:

26

Inhibitors & Agonists

2

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 [2] and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
    Shikonin
  • HY-103617
    PKM2-IN-1
    25+ Cited Publications

    		 Pyruvate Kinase Cancer
    PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM .
    PKM2-IN-1
  • HY-B0404A
    Benserazide hydrochloride
    5+ Cited Publications

    Ro 4-4602 hydrochloride

    		 Pyruvate Kinase Neurological Disease Cancer
    Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma [2] .
    Benserazide hydrochloride
  • HY-121275
    Benserazide
    5+ Cited Publications

    Ro 4-4602

    		 Pyruvate Kinase Neurological Disease Cancer
    Benserazide is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide is also a PKM2 inhibitor. Benserazide directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide can be used for the study of Parkinson's disease and melanoma [2] .
    Benserazide
  • HY-157913
    PKM2-IN-6

    		Pyruvate Kinase Apoptosis Cancer
    PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer .
    PKM2-IN-6
  • 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 [2].
    METTL1-WDR4-IN-1
  • HY-148615
    NPD10084

    		Pyruvate Kinase Cancer
    NPD10084 is a pyruvate kinase PKM2 inhibitor that inhibits non-glycolytic signaling in cancer cells. NPD10084 disrupts the interaction between PKM2 and β-catenin or STAT3 and inhibits downstream signaling. NPD10084 has antiproliferative activity against colorectal cancer cells in vitro and in vivo .
    NPD10084
  • HY-N2552
    Vitamin K5 hydrochloride

    		Pyruvate Kinase Bacterial Fungal Apoptosis Infection Cancer
    Vitamin K5 hydrochloride is a photosensitizer and a antimicrobial agent. Vitamin K5 hydrochloride is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 hydrochloride induces apoptosis of colon 26 cells. Vitamin K5 hydrochloride can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages [2] .
    Vitamin K5 hydrochloride
  • HY-B1814
    Vitamin K5

    Synkamin; Synkamin base

    		 Pyruvate Kinase Bacterial Fungal Apoptosis Infection Cancer
    Vitamin K5 (Synkamin) is a photosensitizer and a antimicrobial agent. Vitamin K5 is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 induces apoptosis of colon 26 cells. Vitamin K5 can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages [2] .
    Vitamin K5
  • HY-155850
    CIAC001

    		Pyruvate Kinase Neurological Disease
    CIAC001 is a Pyruvate Kinase PKM2 inhibitor with anti-neuroinflammatory activity. CIAC001 inhibits LPS-induced proinflammatory nitric oxide (NO) production and protects immunologically active BV-2 cells (IC50=2.5 μM). CIAC001 also has anti-neuroinflammation in mouse models and inhibits chronic morphine-induced addiction .
    CIAC001
  • HY-B0404AR
    Benserazide hydrochloride (Standard)

    Ro 4-4602 hydrochloride (Standard)

    		 Reference Standards Pyruvate Kinase Neurological Disease Cancer
    Benserazide hydrochloride (Standard) (Serazide (Standard)) is the analytical standard of Benserazide hydrochloride (HY-B0404A). This product is intended for research and analytical applications. Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma [2] .
    Benserazide hydrochloride (Standard)
  • 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 [2] and can also inhibit TNF-α and NF-κB pathway . Shikonin decreases exosome secretion through the inhibition of glycolysis . Shikonin inhibits AIM2 inflammasome activation .
    Shikonin (Standard)
  • HY-W587878
    Thujopsene

    		Cytochrome P450 Pyruvate Kinase Fungal Apoptosis Insecticide Infection Cancer
    Thujopsene is the inhibitor for cytochrome P450, that inhibits CYP2B6, CYP3A4, CYP2C19, CYP2C8, CYP2C9 with IC50s of 1.3, 12.6, 13.6, 29.8, and 44.9 μM, respectively. Thujopsene binds to PKM2, inhibits the metabolism pathway of cancer cell, induces apoptosis in MKN45, thereby exhibiting antitumor efficacy. Thujopsene exhibits anti-termite and antifungal activities through autoxidation [2] .
    Thujopsene
  • HY-168883
    PKM2 modulator 2

    		Apoptosis Pyruvate Kinase Cancer
    PKM2 modulator 2 (compound C599) is a potent PKM2 inhibitor. PKM2 modulator 2 shows antiproliferative activity. PKM2 modulator 2 induces apoptosis. PKM2 modulator 2 has the potential for the research of glioblastoma .
    PKM2 modulator 2
  • HY-B0404AS
    Benserazide-d3 hydrochloride

    Ro 4-4602-d3 hydrochloride

    		 Isotope-Labeled Compounds Pyruvate Kinase Neurological Disease Cancer
    Benserazide-d3 (hydrochloride) is the deuterium labeled Benserazide hydrochloride (HY-B0404A). Benserazide hydrochloride (Serazide) is an aromatic L-amino acid decarboxylase (AADC) and L-DOPA decarboxylase inhibitor. Benserazide hydrochloride is also a PKM2 inhibitor. Benserazide hydrochloride directly binds to and blocks PKM2 enzyme activity, leading to inhibition of aerobic glycolysis concurrent up-regulation of OXPHOS. Benserazide hydrochloride can be used for the study of Parkinson's disease and melanoma [2] .
    Benserazide-d3 hydrochloride
  • HY-178748
    PKM2-IN-12

    		Pyruvate Kinase Apoptosis Endogenous Metabolite Reactive Oxygen Species (ROS) Cancer
    PKM2-IN-12 is an orally active PKM2 inhibitor with an IC50 of 10 nM. PKM2-IN-12 inhibits COLO-205 cell proliferation and migration, arrests the cell cycle, and induces apoptosis. PKM2-IN-12 significantly reduces cellular levels of lactate, pyruvate, and ROS. PKM2-IN-12 directly kills cancer cells and restores disrupted gut microbiota balance in mice model. PKM2-IN-12 can be used to study colorectal cancer .
    PKM2-IN-12
  • HY-170577
    PKM2-IN-8

    		Pyruvate Kinase Apoptosis Cancer
    PKM2-IN-8 (Compound 9b) is a pyruvate kinase M2 (PKM2) inhibitor (IC50 = 0.31 μM). PKM2-IN-8 has potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 can induce early apoptosis and reduce lactate levels. PKM2-IN-8 can be used for the research of glioblastoma .
    PKM2-IN-8
  • HY-178441
    PKM2-IN-11

    		Pyruvate Kinase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin Metabolic Disease Cancer
    PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer .
    PKM2-IN-11
  • HY-168882
    PKM2 modulator 1

    		Apoptosis Pyruvate Kinase Cancer
    PKM2 modulator 1 (compound C998) is a potent PKM2 inhibitor. PKM2 modulator 1 shows antiproliferative activity. PKM2 modulator 1 induces apoptosis. PKM2 modulator 1 has the potential for the research of glioblastoma .
    PKM2 modulator 1
  • 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 .
    MTP
  • HY-172881
    PKM2-IN-10

    		Pyruvate Kinase Cancer
    PKM2-IN-10 (Compound 16) is a PKM2 inhibitor. PKM2-IN-10 inhibits the proliferation of A549 and HCC1833 cell lines with IC50 of 3.36 μM and 9.20 μM, respectively. PKM2-IN-10 exhibits antitumor activity in human non-small cell lung cancer (NSCLC) and mouse lung adenocarcinoma models. PKM2-IN-10 can be used in lung cancer research .
    PKM2-IN-10
  • HY-N2552R
    Vitamin K5 hydrochloride (Standard)

    		Reference Standards Pyruvate Kinase Bacterial Fungal Apoptosis Infection Cancer
    Vitamin K5 (hydrochloride) (Standard) is the analytical standard of Vitamin K5 (hydrochloride). This product is intended for research and analytical applications. Vitamin K5 hydrochloride is a photosensitizer and a antimicrobial agent. Vitamin K5 hydrochloride is a specific PKM2 inhibitor with IC50 values of 28, 191 and 120 μM for PKM2, PKM1 and PKL. Vitamin K5 hydrochloride induces apoptosis of colon 26 cells. Vitamin K5 hydrochloride can be used for the research of infection and cancer, and it also can be used as a preservative for pharmaceuticals, foods, and beverages[1][2][3].
    Vitamin K5 hydrochloride (Standard)
  • 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 [2].
    METTL1-WDR4-IN-1 TFA
  • HY-103617R
    PKM2-IN-1 (Standard)

    		Reference Standards Pyruvate Kinase Cancer
    PKM2-IN-1 (Standard) is the analytical standard of PKM2-IN-1 (HY-103617). This product is intended for research and analytical applications. PKM2-IN-1 (compound 3k) is a pyruvate kinase M2 (PKM2) inhibitor with an IC50 of 2.95 μM .
    PKM2-IN-1 (Standard)
  • 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 .
    PKM2-IN-13
  • 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

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: