Catalog No.
Product Name
Application
Product Information
Citations
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PKR Activator
(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. -
PKR Activator
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. -
PKM2 Activator
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. -
PKM2 Activator
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. -
PK Activator
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. -
Pyruvate Kinase Activator
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. -
PK-R Activator
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. -
PKM2 Inhibitor
PKM2-IN-4 is a selective inhibitor of pyruvate kinase M2 (PKM2), exhibiting an IC50 of 0.35 μM. This compound is known to regulate pyruvate-dependent respiration and promotes mitochondrial H2O2 production, impacting the efficiency of the electron transport system. It serves as a valuable tool in research focused on metabolism, cancer biology, and oxidative stress. -
PKM2 Inhibitor
PKM2-IN-9 is a selective inhibitor of pyruvate kinase M2 (PKM2), achieving an inhibition rate of 75% at a concentration of 50 μM. This compound is of significant interest in cancer research, as it regulates metabolic pathways essential for tumor growth and survival. PKM2-IN-9 can be utilized to explore the role of PKM2 in cellular processes and as a potential therapeutic target in various types of cancer. -
PKM2 Activator
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. -
PKR Activator
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. -
Elk3 Inhibitor
Alkannin is a selective inhibitor of tumor-specific pyruvate kinase-M2 (PKM2), demonstrating potent activity without affecting PKM1 or pyruvate kinase-L (PKL). This compound has potential applications in cancer research, serving as a valuable tool for studying metabolic alterations in tumors and developing anticancer strategies. Alkannin's specificity for PKM2 highlights its utility in targeted therapeutic approaches in oncology. -
hPK-M2 Activator
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. -
PKM2 Agonist
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. -
Pyruvate Kinase Inhibitor
PKM2-IN-5 is a selective inhibitor of pyruvate kinase M2 (PKM2), a critical enzyme involved in cellular energy metabolism. This compound exhibits potential for modulating glucose metabolism and influencing tumorigenesis by inhibiting PKM2 activity. PKM2-IN-5 is valuable for research applications in cancer biology and metabolic disorders, providing insights into the role of PKM2 in various cellular processes. -
Pyruvate Kinase Stimulator
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. -
Inverse RAR Inhibitor
BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist that enhances nuclear corepressor interaction with RARs, effectively inhibiting retinoic acid-induced differentiation. This compound serves as a valuable tool in research applications focused on RAR signaling pathways and their regulatory mechanisms. Additionally, BMS493 features an alkyne group, enabling its use in click chemistry through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating diverse labeling and conjugation strategies. -
Retinol Derivative
Hydroxypinacolone retinoate (HPR) is a retinol derivative that selectively binds to retinoic acid receptors (RARs). Its primary biological activity includes promoting cellular turnover and collagen synthesis, making it relevant in anti-aging research. HPR is often studied for its potential to improve skin texture and reduce the appearance of fine lines and wrinkles, particularly when used in conjunction with other retinoids. -
RAR Antagonist
AGN 193109 is a potent retinoic acid receptor (RAR) antagonist, exhibiting binding affinities of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, respectively. This compound is utilized in research to investigate RAR signaling and its implications in various biological processes. Additionally, AGN 193109 contains an alkyne group that enables its use in click chemistry applications through copper-catalyzed azide-alkyne cycloaddition (CuAAc). Its therapeutic potential includes serving as an antidote for retinoic acidosis, alleviating skin and mucosal toxicity associated with excess retinoic acid. -
RXR-Selective Agonist
SR11237 is a potent retinoid X receptor (RXR)-selective agonist that exhibits no activity on retinoic acid receptors (RARs). This compound efficiently induces the formation of RXR/RXR homodimers and effectively transactivates reporter genes containing RXR-responsive elements. It is valuable for research in areas related to nuclear hormone signaling pathways and RXR-mediated transcriptional regulation. -
RAR-α/RAR-β Agonist
Ch55 is a potent agonist of the retinoic acid receptors RAR-α and RAR-β. It demonstrates a high affinity for these receptors while exhibiting low binding affinity for cellular retinoic acid binding protein (CRABP). Ch55 effectively induces differentiation in HL60 cells, with an EC50 of 200 nM. This compound is particularly valuable in cancer research applications, offering insights into retinoid-mediated pathways in tumorigenesis and cell differentiation. -
RXR Agonist
CD3254 is a potent and selective retinoid-X-receptor (RXR) agonist that plays a crucial role in modulating gene expression related to lipid metabolism, apoptosis, and differentiation. Its activation of RXR can influence signaling pathways involved in various diseases, making it a valuable tool for research in metabolic disorders and cancer. CD3254 is suitable for studies investigating RXR's role in cellular processes and its potential therapeutic applications. -
RARγ Antagonist
MM11253 is a potent and selective antagonist of Retinoic Acid Receptor gamma (RARγ) with an IC50 of 44 nM. It exhibits minimal activity against RARα, RARβ, and RXRα. This compound effectively inhibits the growth-promoting effects of RARγ-selective agonists, making it a valuable tool for research focused on cancer biology and metabolism involving RARγ signaling pathways. -
RXR Antagonist
PA452 is a specific antagonist of the retinoic X receptor (RXR). It effectively inhibits the actions of retinoic acid (RA) on the differentiation of Th1 and Th2 cells. This compound is relevant for research focusing on immune response modulation and the therapeutic potential in various inflammatory and autoimmune conditions. -
RARα Agonist
BMS 753 is an isotype-selective retinoic acid receptor α (RARα) agonist, exhibiting a Ki of 2 nM. This compound modulates gene expression linked to cellular differentiation, proliferation, and apoptosis through RARα activation. Its selective action makes BMS 753 valuable for investigating the role of RARα in various biological processes and potential therapeutic areas, including cancer research and regenerative medicine. -
RAR-beta/gamma Antagonist
CD2665 is a selective antagonist of retinoic acid receptors RAR-β and RAR-γ, exhibiting Kd values of 306 nM and 110 nM for each receptor, respectively. This compound is beneficial for studying the modulation of retinoic acid signaling pathways implicated in various biological processes. CD2665 is suitable for applications in cancer research, developmental biology, and pharmacological studies involving retinoid signaling. -
RARβ agonist
CD2314 is a potent and selective agonist of the RARβ receptor, exhibiting a Kd of 195 nM in S91 melanoma cells. This compound modulates retinoic acid signaling pathways, promoting cellular differentiation and apoptosis. CD2314 is valuable for investigating the roles of RARβ in cancer biology and other research applications related to retinoid signaling. -
RXR Modulater
LG100754 is an RXR modulator that functions as an antagonist of RXR:RXR homodimers while acting as an agonist for RXR:PPARα and RXR:PPARγ heterodimers. This compound serves as an insulin sensitizer, exerting its biological effects through receptor interactions involving the retinoid X receptor (RXR). Its unique modulation of RXR dimers makes LG100754 a valuable tool for research in metabolic disorders and cellular signaling pathways. -
RARα Antagonist
ER 50891 is a RARα antagonist that counteracts the inhibitory effects of all-trans retinoic acid (ATRA) on metabolic activity and proliferation in MC3T3-E1 preosteoblasts. This compound effectively rescues ATRA-reduced osteocalcin (OCN) expression and enhances extracellular matrix mineralization, while simultaneously suppressing alkaline phosphatase (ALP) activity. ER 50891 is applicable for research focused on osteoporosis and the mechanisms of ATRA-induced inhibition of osteoblastogenesis. -
RARβ Agonist
BMS641 is a selective RARβ agonist with a high affinity for the RARβ receptor (Kd of 2.5 nM), exhibiting over 100-fold selectivity compared to RARα (Kd of 225 nM) and RARγ (Kd of 223 nM). This compound is valuable in investigating the role of RARβ in various biological processes and may have implications in cancer research and differentiation studies. Its specificity makes BMS641 a useful tool for elucidating RARβ-mediated signaling pathways. -
RARβ2 Agonist
KCL-286 is a potent retinoic acid receptor (RAR) β2 agonist, with an EC50 of 1.9 nM, demonstrating high selectivity over RAR α and RAR γ (EC50 = 26 nM and 11 nM, respectively). This compound activates RARβ2 specifically in injured neurons, promoting axonal regeneration in the spinal cord and sensory nerves by altering the inhibitory environment in the central nervous system. KCL-286 also modulates neuroinflammation and extracellular matrix components, influencing the expression of chondroitin sulfate proteoglycans through neuronal secretion of decorin to facilitate myelination and enhance axonal growth. It is relevant for research applications in spinal cord injury and traumatic nerve injury studies. -
RARbeta2 Agonist
AC-261066 is a selective agonist of the retinoic acid receptor beta2 (RARbeta2) with high potency and oral bioavailability, exhibiting a pEC50 of 8.0. This compound is utilized in research to investigate the biological functions of RARbeta2 and its implications in cellular differentiation, growth, and apoptosis. Its isoform-selective action makes it a valuable tool for studies aimed at understanding retinoid signaling pathways and their therapeutic potential. -
RXR Agonist
HX600 is a synthetic agonist targeting the retinoid X receptor (RXR) heterodimer complex. It demonstrates neuroprotective properties by preventing ischemia-induced neuronal damage, making it valuable for research into neurodegenerative disorders and ischemic injury. Additionally, HX600 exhibits oral bioavailability, enhancing its potential for in vivo studies. -
RXRα Antagonist
XS-060 is a potent RXRα antagonist that functions by disrupting the interaction between phosphorylated RXRα (pRXRα) and PLK1, leading to RXRα-dependent mitotic arrest. This compound specifically targets the centrosomal interaction of p-RXRα and PLK1 without interfering with RXRα heterodimerization with RARγ. XS-060 is primarily utilized in cancer research to explore mechanisms of mitotic regulation and potential therapeutic applications in oncology. -
RARγ Agonist
BMS961 is a selective agonist of the retinoic acid receptor-γ (RARγ). It demonstrates potent anti-inflammatory activity, making it a valuable tool for research into inflammatory diseases and related pathways. This compound can be utilized in studies aimed at understanding RARγ-mediated signaling and its implications in therapeutic contexts. -
RAR Neutral Antagonist
AGN 192870 is a selective RAR neutral antagonist that demonstrates binding affinities (Kd) of 147 nM for RARα, 33 nM for RARβ, and 42 nM for RARγ. It exhibits inhibitory concentrations (IC50) of 87 nM for RARα and 32 nM for RARγ while showcasing partial agonism at RARβ. Additionally, AGN 192870 features an alkyne group, facilitating its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, providing utility in various chemical biology applications. -
Nuclear Retinoic Acid Receptor γ Inhibitor
BMS270394 is a selective inhibitor of the nuclear retinoic acid receptor gamma (RAR-γ), exhibiting an EC50 of 30 nM for human RAR-γ. This compound demonstrates potent activity against RAR-β with an EC50 of 400 nM. BMS270394 is valuable in research applications focused on gene regulation, developmental biology, and potential therapeutic interventions related to retinoid signaling pathways. -
RARα Antagonist
RARα antagonist 1 is a selective antagonist of the retinoic acid receptor α (RARα), functioning at an IC50 of 4.6 nM. This compound disrupts RARα-mediated signaling, making it a valuable tool for studying the role of this receptor in various biological processes. Its applications extend to cancer research, developmental biology, and investigations of metabolic disorders, where modulation of retinoic acid signaling is crucial. -
Retinoid X Receptor Modulator
RXR Antagonist 1 is a selective retinoid X receptor (RXR) modulator demonstrating potent antagonistic activity, with a pA2 value of 8.06. This compound is particularly relevant in research pertaining to type 2 diabetes, offering insights into RXR-related pathways and their impact on metabolic processes. Its effective inhibition of RXR activity makes it a valuable tool for exploring therapeutic interventions in metabolic disorders. -
RAR/RXR Inhibitor
RXR Antagonist 5 is a selective retinoic acid X receptor (RXR) inhibitor, designed to modulate RXR activity. It effectively disrupts RXR signaling pathways, making it a valuable tool for investigating the role of RXR in various biological processes. This compound can be utilized in research applications focused on cancer biology, metabolism, and developmental studies, providing insights into RXR-mediated physiological functions. -
RARγ Nuclear Receptor Agonist
IRX5010 is a selective agonist of the RARγ nuclear receptor. It has been shown to inhibit the in vivo growth of EMT-6 triple-negative breast cancer cells, making it a valuable tool for cancer research. This compound is particularly useful for studying the role of RARγ in tumor biology and exploring therapeutic strategies targeting this receptor. -
RARs Agonist
Arotinoid functions as a highly potent agonist of retinoic acid receptors (RARs). Known for its antipsoriatic effects, Arotinoid exhibits antipapilloma activity with an ED50 of 0.05 mg/kg. This compound is valuable in research related to skin carcinomas, contributing to the understanding of retinoid biology and potential therapeutic applications. -
RAR/RXR Agonist
Fluorobexarotene is a potent agonist of retinoid-X-receptors (RXR), exhibiting a Ki value of 12 nM and an EC50 value of 43 nM for the RXRα receptor. This compound demonstrates a binding affinity for RXR that is 75% greater than that of Bexarotene. Fluorobexarotene is valuable for research applications targeting RXR-mediated signaling pathways, which are implicated in various biological processes including cellular differentiation and metabolism. -
RAR/RXR Activator
Viaminate is a potent RAR/RXR activator, functioning as a derivative of Retinoic acid. It plays a crucial role in regulating gene expression involved in cellular differentiation and proliferation. This compound is primarily utilized in research on severe acne and various keratinization disorders, providing insights into the underlying molecular mechanisms and potential therapeutic avenues. -
RXR Agonist
16α-Hydroxytrametenolic acid is a natural triterpene that selectively functions as an agonist for the retinoid X receptor (RXR). This compound has demonstrated potential in modulating RXR activity, thereby influencing pathways involved in lipid metabolism, cell differentiation, and apoptosis. Its applications in research include studying RXR's role in cancer biology and metabolic disorders, providing valuable insights into therapeutic approaches targeting these pathways. -
RAR/RXR Inhibitor
NBD-125 is a potent RAR/RXR inhibitor that modulates retinoic acid receptor signaling. It functions as an RXRα activator, demonstrating an IC50 of 31.10 μM in KM12C cells. This compound is valuable for research applications involving the regulation of gene expression and signaling pathways associated with nuclear receptor activity. -
Retinoic Acid Analogue
DC360 is a synthetic retinoid analogue of all-trans retinoic acid (ATRA) that primarily targets retinoic acid receptors (RARs), particularly RARβ. It plays a significant role in modulating gene expression and is instrumental in the study of retinoid signaling pathways. Researchers can utilize DC360 to explore its effects on cellular differentiation and proliferation in various biological contexts. -
Retinoic Acid Receptor Agonist
ALRT1550 is a potent selective agonist of the retinoic acid receptors (RARs), exhibiting Kd values between 1-4 nM. This compound demonstrates significant anti-proliferative effects, evidenced by an IC50 of 0.22 nM in UMSCC-22B squamous carcinoma cells. In vivo studies in mouse tumor xenograft models have shown ALRT1550 to inhibit tumor growth in a dose-dependent manner, achieving up to 89% inhibition at maximum doses. This reagent is highly relevant for research focused on cancer biology and therapeutic applications targeting the retinoic acid signaling pathway. -
RXR Antagonist
RXR Antagonist 2 is a potent antagonist of retinoid X receptors (RXR), exhibiting a Ki value of 0.391 μM and a Kd of 0.281 μM. This compound is valuable for investigating RXR-related biological processes and diseases, making it a useful tool in molecular biology and pharmacological research. Its ability to inhibit RXR activity allows for studies on its role in various signaling pathways and therapeutic interventions. -
RXR Agonist
NEt-iFQ is a fluorescent retinoid X receptor (RXR) agonist that exhibits potent solvatochromic properties. This compound selectively binds to the RXR-ligand binding pocket, producing fluorescence, which facilitates studies on RXR-mediated signaling pathways. It is useful in research applications involving nuclear receptor activation and cellular imaging.
