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- Cat. No.
- A15895
DASA-58
DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.
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- Cat. No.
- A16279
TEPP-46
Synonyms: ML-265
TEPP-46 is a potent and selective activator of recombinant pyruvate kinase M2 (PKM2) with half-maximum activating concentration (AC50 value) of 92 nM, and little or no activity versus PKM1, PKL and PKR.
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- Cat. No.
- A22367
Mitapivat
Mitapivat is a pyruvate kinase isoenzyme M2 (PKM2) activator.
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- Cat. No.
- A25392
BEPP hydrochloride
BEPP hydrochloride is a potent inducer of double-stranded RNA-dependent protein kinase (PKR), demonstrating significant antiviral properties. It effectively inhibits the proliferation of human lung cancer cell lines that overexpress PKR, leading to apoptosis and the activation of caspase-3 in responsive cells. Furthermore, BEPP hydrochloride significantly hinders the replication of vaccinia virus, making it a valuable compound for research applications in cancer and virology studies.
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- Cat. No.
- A32181
Bozepinib
Bozepinib is an activator of PKR (RNA-dependent protein kinase) that potently inhibits the HER-2 signaling pathway along with JNK and ERK kinases. This compound induces PKR-mediated apoptosis, enhancing the apoptotic, autophagic, and senescent processes, particularly in synergy with IFNα. Additionally, Bozepinib exhibits significant in vivo antitumor and antimetastatic effects in xenograft models, making it a valuable reagent for cancer research applications.
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- Cat. No.
- A77400
Tebapivat
Synonyms: AG-946; PKR activator 2
Tebapivat is a potent activator of pyruvate kinase-R (PKR), playing a critical role in enhancing glycolytic flux and energy metabolism. Its ability to stimulate PKR makes it valuable in research on metabolic disorders and cancer, where glycolysis is often dysregulated. Tebapivat can be utilized to investigate the effects of PKR activation on cellular energy production and related biochemical pathways.
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- Cat. No.
- A77401
PKM2 activator 2
PKM2 activator 2 is a potent activator of pyruvate kinase M2 (PKM2) with an AC50 value of 66 nM. This compound effectively enhances PKM2 activity, facilitating the restoration of normal glycolytic metabolism in various cellular models. It is valuable for research applications focusing on cancer metabolism and cellular energy regulation, offering insights into metabolic reprogramming in tumors.
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- Cat. No.
- A77402
Etavopivat
Synonyms: FT-4202
Etavopivat is a selective erythrocyte pyruvate kinase (PKR) activator that enhances glycolytic flux in red blood cells. It exhibits significant antisickling effects, making it a valuable tool for investigating sickle cell disease and other hemoglobinopathies. This compound is of interest in research aimed at improving red blood cell function and mitigating the complications associated with abnormal hemoglobin disorders.
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- Cat. No.
- A77406
PKM2 activator 5
PKM2 activator 5 is a selective activator of pyruvate kinase M2 (PKM2) with an AC50 value of 0.316 µM. This compound modulates the metabolic pathways of cancer cells by enhancing PKM2 activity, thereby promoting a shift from aerobic to anaerobic metabolism. PKM2 activator 5 has applications in cancer research, particularly in studies focused on metabolic reprogramming and the development of novel therapeutic strategies targeting cancer metabolism.
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- Cat. No.
- A77411
PKR activator 1
PKR Activator 1 is a potent activator of pyruvate kinase-R (PKR), facilitating enhanced glycolytic flux and promoting overall metabolic activity. This compound is instrumental in studies exploring metabolic disorders, cancer metabolism, and the regulation of cellular energy pathways. With its ability to modulate PKR activity, PKR Activator 1 serves as a valuable tool for researchers investigating the role of PKR in various biological contexts.
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- Cat. No.
- A77412
PF-06284674
Synonyms: PKM2 activator 1
PF-06284674 is a potent activator of PKM2, a key enzyme involved in cancer metabolism. This compound enhances the activity of PKM2, promoting metabolic switching and cellular proliferation. It is primarily utilized in cancer research, particularly studies focused on targeting metabolic pathways for therapeutic intervention.
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- Cat. No.
- A77413
ML202
ML202 is a potent allosteric activator of human pyruvate kinase M2 (hPK-M2), designed to enhance the enzyme's activity by modulating the cooperativity of phosphoenolpyruvate (PEP) binding. It specifically influences the PEP binding site with minimal impact on adenosine diphosphate (ADP) binding. This compound is valuable for studying metabolic pathways and cellular energy regulation, making it a useful tool in cancer research and metabolic studies.
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- Cat. No.
- A77414
(Rac)-Etavopivat
Synonyms: (Rac)-FT-4202
(Rac)-Etavopivat is an isomer of Etavopivat and functions as an activator of erythrocyte pyruvate kinase-R (PKR). This compound exhibits the potential to enhance glycolytic flux in erythrocytes, making it valuable for research on sickle cell disease and other hemoglobinopathies. Its oral bioavailability allows for convenient dosing in in vitro and in vivo studies, supporting investigations into erythrocyte metabolism and therapeutic strategies.
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- Cat. No.
- A77415
PKR activator 5
PKR Activator 5 (Compound 18) is a potent activator of pyruvate kinase R (PKR), exhibiting an AC50 of 28 nM. This compound enhances PKR activity, which plays a critical role in regulating glycolysis and energy metabolism. PKR Activator 5 is valuable for research applications aimed at understanding the metabolic pathways associated with PKR and their implications in cancer and metabolic disorders.
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- Cat. No.
- A77416
PKM2 activator 10
PKM2 activator 10 is a selective activator of the pyruvate kinase M2 (PKM2) enzyme, promoting its tetrameric form and enhancing glycolytic activity. This compound demonstrates significant anti-tumor activity, making it a valuable tool in cancer research. Its ability to modulate metabolic pathways provides insights into therapeutic strategies for cancer treatment and metabolic disorders.
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- Cat. No.
- A77417
PKM2 activator 4
PKM2 Activator 4 is a potent activator of the pyruvate kinase M2 (PKM2) enzyme, exhibiting an AC50 value in the range of 1-10 μM. This compound is primarily utilized in cancer research, where modulation of PKM2 activity may influence metabolic pathways involved in tumor growth and cell proliferation. Its role in enhancing PKM2 function makes it a valuable tool for investigating cancer metabolism and potential therapeutic strategies.
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- Cat. No.
- A77418
Mitapivat hemisulfate
Synonyms: AG-348 hemisulfate
Mitapivat hemisulfate is an orally active allosteric activator of pyruvate kinase (PK). This compound enhances enzymatic activity, improves protein stability, and elevates ATP levels across various PKLR genotypes, making it a potential therapeutic option for restoring function in PK-deficient glycolytic pathways. Mitapivat hemisulfate is suitable for research applications focused on PK deficiency and metabolic disorders.
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- Cat. No.
- A77419
Mitapivat hemisulfate sesquihydrate
Synonyms: AG-348 hemisulfate sesquihydrate
Mitapivat hemisulfate sesquihydrate is an orally active allosteric activator of pyruvate kinase (PK). This compound enhances enzymatic activity and protein stability while increasing ATP levels across various PKLR genotypes. Mitapivat is instrumental in studying pyruvate kinase deficiencies and has significant implications for restoring glycolytic pathway activity in affected cells.
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- Cat. No.
- A77420
Mitapivat hydrochloride
Synonyms: AG-348 hydrochloride
Mitapivat hydrochloride is a selective allosteric activator of pyruvate kinase R (PK-R). By enhancing the enzymatic activity of PK-R, it facilitates the conversion of phosphoenolpyruvate to pyruvate, promoting glycolysis and leading to increased ATP production in red blood cells while decreasing levels of 2,3-diphosphoglycerate. This compound shows potential for investigational studies related to pyruvate kinase deficiency and various anemia-related disorders.
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- Cat. No.
- A77424
PKM2 activator 3
PKM2 activator 3 is a potent activator of pyruvate kinase M2 (PKM2), exhibiting an AC50 value of 90 nM. This compound demonstrates favorable Caco-2 permeability, low efflux ratio, and high microsomal stability, making it an advantageous tool for in vitro studies. PKM2 activator 3 is primarily utilized in cancer research, facilitating the investigation of metabolic pathways and potential therapeutic strategies targeting PKM2.
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- Cat. No.
- A77425
PKR activator 4
PKR Activator 4 is a potent activator of pyruvate kinase R (PKR), enhancing its enzymatic activity. This compound demonstrates key biological activity by stimulating glycolytic flux and ATP production, making it instrumental in studies related to energy metabolism and blood disorders. Researchers can utilize PKR Activator 4 to investigate its effects on cellular metabolism and the potential therapeutic implications for metabolic dysfunctions.
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- Cat. No.
- A77427
ML 083
Synonyms: BML283
ML083 is a selective allosteric activator for the tumor-specific isoform of human pyruvate kinase (PK-M2). By modulating the cooperativity of phosphoenolpyruvate (PEP) binding, ML083 enhances PK-M2 activity, making it a valuable tool for studying tumor metabolism. This compound is essential for research applications focusing on cancer biology and metabolic regulation within tumor cells.
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- Cat. No.
- A77428
PKM2 agonist-1
PKM2 agonist-1 is an allosteric activator of pyruvate kinase M2 (PKM2) with a reported AC50 of 77 nM. This compound has been shown to inhibit angiotensin II-induced phenotypic switching in smooth muscle cells, demonstrating significant biological activity in vascular biology. Additionally, PKM2 agonist-1 effectively reduces the incidence of aortic dissection and associated mortality, making it a valuable tool for research in cardiovascular disease and cellular metabolism.
Out of stock
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- Cat. No.
- A77430
2,5-Anhydro-D-glucitol-1,6-diphosphate
2,5-Anhydro-D-glucitol-1,6-diphosphate is an allosteric stimulator of yeast Pyruvate Kinase, enhancing its enzymatic activity. This compound serves as an analogue of 2,5-anhydro-D-mannitol 1,6-bisphosphate, providing insights into the regulatory mechanisms of glycolysis. Its application in biochemical research facilitates the study of metabolic pathways and enzyme kinetics linked to energy production in yeast.
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