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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 .
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 .
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.)
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-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 .
PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway .
Pkm2-in-4 (compound 5C) is a selective inhibitor of PKM2 (IC50=0.35 μM), which regulates pyruvate-dependent respiration and induces mitochondrial H202 production rate and electron transport system coupling .
Benserazide is 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 research of melanoma .
TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe. TEPC466 shows a high degree of selectivity and sensitivity for the detection of PKM2 protein via the AIE effect. EPC466 can be used for the detection of PKM2. TEPC466 is successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. TEPC466 is a useful tool for cancer diagnosis and research .
ZY-2 is a specific fluorescent probe for pyruvate kinase M2(PKM2).ZY-2 can image in PKM2-positive cells in a time- and concentration-dependent manner. ZY-2 can be used for the detection of cancer cells .
ZY-1 is a control molecule of ZY-2 (HY-D1876, a PKM2 fluorescent probe). ZY-1 shows a low fluorescence emission in HeLa, a cervical cancer cell abundant in PKM2 expression .
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 [2].
SAICAR-d 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[1][2].
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 .
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] .
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 .
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent .
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 .
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 .
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 .
Mitapivat (AG-348) is an orally active pyruvate kinase allosteric activator. Mitapivat increases enzymatic activity, protein stability, and ATP levels over a broad range of PKLR genotypes, shows the potential to restore the activity of PK (pyruvate kinase)-deficient glycolytic pathways. Mitapivat can be used in study of PK deficiency [2] .
Cynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM. Cynaroside also is a promising inhibitor for H2O2-induced apoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities .
Cynaroside (Standard) is the analytical standard of Cynaroside. This product is intended for research and analytical applications. Cynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM. Cynaroside also is a promising inhibitor for H2O2-induced apoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities .
TEPC466 is a novel TEPP-46-based aggregation-induced emission (AIE) probe. TEPC466 shows a high degree of selectivity and sensitivity for the detection of PKM2 protein via the AIE effect. EPC466 can be used for the detection of PKM2. TEPC466 is successfully applied in imaging the PKM2 protein in colorectal cancer cells with low toxicity. TEPC466 is a useful tool for cancer diagnosis and research .
ZY-1 is a control molecule of ZY-2 (HY-D1876, a PKM2 fluorescent probe). ZY-1 shows a low fluorescence emission in HeLa, a cervical cancer cell abundant in PKM2 expression .
ZY-2 is a specific fluorescent probe for pyruvate kinase M2(PKM2).ZY-2 can image in PKM2-positive cells in a time- and concentration-dependent manner. ZY-2 can be used for the detection of cancer cells .
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 [2].
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 .
Cynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM. Cynaroside also is a promising inhibitor for H2O2-induced apoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities .
Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2). Alkannin does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin acts as a potential anticancer agent .
Cynaroside (Standard) is the analytical standard of Cynaroside. This product is intended for research and analytical applications. Cynaroside (Luteolin 7-glucoside) is a flavonoid compound that exhibits anti-oxidative capabilities. Cynaroside is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 32 nM. Cynaroside also is a promising inhibitor for H2O2-induced apoptosis, has cytoprotection against oxidative stress-induced cardiovascular diseases. Cynaroside also has antibacterial, antifungal and anticancer activities, antioxidant and anti-inflammatory activities .
PKM2 protein catalyzes the final step of glycolysis, transferring a phosphoryl group from PEP to ADP to generate ATP. In the nucleus, transcriptional activation of PKM2 contributes to cancer progression, promoting cell proliferation and tumorigenesis. PKM2 is also involved in caspase-independent cell death in tumors. PKM2 Protein, Mouse (sf9, His) is the recombinant mouse-derived PKM2 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of PKM2 Protein, Mouse (sf9, His) is 530 a.a., with molecular weight of ~59 kDa.
PKM2 Protein, Human (420 a.a, His) is a multifunctional protein, is exclusively expressed in embryonic and adult dividing/tumor cells. PKM2 can catabolize glucose and involved in many nonglycolytic pathways.
PKM2 protein catalyzes the final step of glycolysis, transferring a phosphoryl group from PEP to ADP to generate ATP. In the nucleus, transcriptional activation of PKM2 contributes to cancer progression, promoting cell proliferation and tumorigenesis. PKM2 is also involved in caspase-independent cell death in tumors. PKM2 Protein, Mouse (Baculovirus, His-Myc) is the recombinant mouse-derived PKM2 protein, expressed by Sf9 insect cells , with N-10*His, C-Myc labeled tag. The total length of PKM2 Protein, Mouse (Baculovirus, His-Myc) is 531 a.a., with molecular weight of ~61.8 kDa.
SAICAR-d 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[1][2].
PKM2 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 58 kDa, targeting to PKM2. It can be used for WB assays with tag free, in the background of Human, Mouse, Rat, Monkey.