Catalog No.
Product Name
Application
Product Information
Citations
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IDH Inhibitor
(S,S)-GSK321 is a selective inhibitor of isocitrate dehydrogenase (IDH), specifically targeting mutated forms of the enzyme. This compound exhibits significant anti-cancer activity by disrupting the metabolic pathways in cells with IDH mutations. It is primarily utilized in research focused on cancer therapeutics and metabolic disease modeling. -
IDH Inhibitor
Lanisidenib is an isocitrate dehydrogenase (IDH) inhibitor that displays potent antineoplastic activity. By targeting abnormal IDH enzymes, it disrupts metabolic pathways involved in tumor growth and survival. This compound is applicable in research focused on cancer metabolism and therapeutic strategies for IDH-mutated malignancies. -
IDH1 Inhibitor
IDH1 Inhibitor 5 is an inhibitor of isocitrate dehydrogenase 1 (IDH1), targeting both wild-type and mutant forms of the enzyme. It demonstrates potent biological activity with IC50 values of 64.4 nM in MOG cells and 34.9 nM in glioma cells expressing the exogenous mutant IDH1 R132H protein. This compound is valuable for research applications focused on glioma and other IDH1-related oncogenic processes. -
IDH2 R140Q Mutant Inhibitor
IDH2R140Q-IN-2 is a selective inhibitor targeting the IDH2 R140Q mutant with an IC50 of 29 nM. This compound effectively reduces the production of D2HG in TF-1 cell lines expressing the mutant IDH2 R140Q, demonstrating an IC50 of 10 nM. IDH2R140Q-IN-2 is useful for studying the role of mutant IDH2 in acute myeloid leukemia (AML) and can significantly suppress D2HG levels in tumor tissue. -
IDH2R140Q Inhibitor
IDH2R140Q-IN-1 is a selective inhibitor of the IDH2R140Q mutant isoform, demonstrating a potent inhibitory effect with an IC50 of 6.1 nM. This compound is primarily utilized in research focused on acute myeloid leukemia, contributing to the understanding of IDH2-driven oncogenesis and potential therapeutic strategies. Its application in preclinical studies may facilitate the development of targeted treatments aimed at malignancies associated with IDH mutations. -
IDH1-mutant Inhibitor
IHMT-IDH1-053 is a highly selective and irreversible inhibitor of IDH1 R132H mutants, with an IC50 of 4.7 nM. It demonstrates pronounced selectivity against IDH1 wild-type and various IDH2 isoforms. IHMT-IDH1-053 effectively inhibits the production of 2-hydroxyglutarate (2-HG) in IDH1 R132H mutant transfected 293T cells, achieving an IC50 of 28 nM. Additionally, this compound blocks the proliferation of HT1080 cell lines and primary acute myeloid leukemia (AML) cells harboring IDH1 R132 mutants, providing valuable insights for therapeutic target validation in IDH1-mutant driven malignancies. -
IDH2/R140Q Inhibitor
CP-17 is a selective inhibitor of the IDH2/R140Q mutation, demonstrating an IC50 of 40.75 nM. It exhibits over 55-fold selectivity against wild-type IDH2, effectively reducing D-2-HG levels in TF-1 cells harboring the IDH2/R140Q mutation. Additionally, CP-17 effectively reverses the cellular differentiation blockade associated with the R140Q mutation, making it a valuable tool for research in acute myeloid leukemia (AML). -
IDH2 Mutant Inhibitor
TQ05310 is an orally bioavailable inhibitor of IDH2 mutants, specifically targeting IDH2-R140Q (IC50=136.9 nM) and IDH2-R172K (IC50=37.9 nM). It effectively inhibits the enzymatic activity of these mutants, resulting in reduced levels of 2-hydroxyglutarate (2-HG) and promoting differentiation in affected cells. TQ05310 is valuable for research applications focused on acute myeloid leukemia. -
IDH1 R132H Inhibitor
ML309 is a potent and selective inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H) with an IC50 of 96 nM. It acts as a competitive inhibitor of α-ketoglutarate (α-KG), exhibiting a Ki value of 156 nM while demonstrating minimal inhibition of wild-type IDH1. In in vitro studies, ML309 effectively decreases the production of the oncometabolite 2-hydroxyglutarate (2-HG) in U87MG cells. This compound serves as a valuable chemical probe for investigating the role of mutant IDH1 in cancer progression and therapeutic response. -
GSK321 Negative Control
GSK990 is an inactive mutant isocitrate dehydrogenase 1 (IDH1) inhibitor that exhibits no significant inhibitory activity against either wild-type or mutant IDH1/IDH2 enzymes. This compound is primarily utilized as a negative control in research studies involving the active IDH1 inhibitor GSK321. GSK990 is particularly relevant for investigations focusing on acute myeloid leukemia, enabling researchers to validate the specificity and efficacy of IDH1-targeted treatments. -
Mutant IDH1 Inhibitor
MRK-A is a selective inhibitor of mutant IDH1, demonstrating a potent IC50 value of 5 nM. By effectively inhibiting the production of 2-hydroxyglutarate (2-HG), MRK-A exhibits significant anti-cancer activity specifically against brain tumors. This compound is suited for research applications aimed at understanding the role of mutant IDH1 in tumorigenesis and exploring therapeutic strategies for brain cancer treatment. -
mIDH1 Inhibitor
mIDH1-IN-1 is a selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1) and exhibits an IC50 of 961.5 nM. This compound effectively reduces intracellular 2-hydroxyglutarate (2-HG) levels in HT1080 cells, demonstrating an EC50 of 208.6 ± 8.0 nM. Additionally, mIDH1-IN-1 displays significant anti-proliferative effects in IDH1 mutant U-87 cells, with an IC50 of 41.8 nM. This antitumor agent is valuable for research on IDH1-mutated solid tumors. -
mIDH2 Inhibitor
SH1573 is an orally active inhibitor of mutant isocitrate dehydrogenase 2 (mIDH2). It exhibits a strong and selective inhibitory effect on the mIDH2 R140Q variant, with an IC50 value of 4.78 nmol/L, effectively reducing the production of the oncogenic metabolite 2-hydroxyglutarate (2-HG) in various biological contexts, including animal models, cell lines, and tumors. SH1573 is designed for research applications in acute myeloid leukemia (AML) to investigate potential therapeutic strategies targeting mIDH2 mutations. -
IDH1-R132H Inhibitor
BRD2879 is a selective inhibitor of the mutant isocitrate dehydrogenase 1 (IDH1-R132H), exhibiting an IC50 of 0.05 µM against this target. This compound effectively reduces levels of (R)-2-hydroxyglutarate (R-2HG), a metabolite associated with IDH mutations in various cancers. BRD2879 is valuable for research investigating IDH-related tumorigenesis and therapeutic strategies in malignant conditions driven by this mutation. -
mIDH1 Inhibitor
AGI-14100 is a potent mIDH1 inhibitor, exhibiting an IC50 of 6 nM. This compound has been carefully optimized to ensure metabolic stability and oral bioavailability, while minimizing human pregnane X receptor (hPXR) activation. AGI-14100 serves as a valuable tool for investigating the role of mutant isocitrate dehydrogenase 1 (mIDH1) in various cancer types, particularly those with IDH1 mutations. Its development enhances the understanding of mIDH1 inhibitors and their therapeutic potential in oncology research. -
Mutant IDH1 Inhibitor
Mutant IDH1-IN-3 is a selective allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1), demonstrating an IC50 of 13 nM specifically for the R132H IDH1 variant. By inhibiting this enzyme, Mutant IDH1-IN-3 effectively reduces the production of D-2-hydroxyglutaric acid (2HG) in cellular models. This compound is particularly valuable in cancer research, providing insights into metabolic alterations and therapeutic strategies targeting IDH1 mutations. -
IDH Inhibitor
Crelosidenib (gentisate) is a selective oral inhibitor of mutant isocitrate dehydrogenase (IDH) enzymes, specifically targeting IDH1 R132H (IC50 of 6.27 nM), IDH1 R132C (IC50 of 3.71 nM), IDH2 R140Q (IC50 of 36.9 nM), and IDH2 R172K (IC50 of 11.5 nM). It demonstrates decreased activity against wild-type IDH enzymes. Crelosidenib is primarily utilized in research focusing on metabolic dysregulation and oncogenic pathways associated with IDH mutations in various cancers. -
IDH1/2 Modulator
AGI-12026 is a brain-penetrant dual inhibitor targeting mutant isocitrate dehydrogenase 1 and 2 (IDH1/2). It acts as an allosteric modulator, demonstrating partial inhibition of the IDH1-R132H homodimer. This compound is suitable for research applications related to glioma and provides a valuable tool for studying the role of mutant IDH enzymes in cancer biology. -
Lactate Dehydrogenase Inhibitor
Galloflavin is a potent lactate dehydrogenase (LDH) inhibitor, specifically targeting both LDH-A and LDH-B with calculated inhibition constants of 5.46 μM and 15.06 μM, respectively. By inhibiting LDH, Galloflavin disrupts glycolysis and ATP production, thereby hindering the proliferation of cancer cells. This compound is valuable for research applications focused on metabolic regulation and cancer therapeutics. -
Lactate Dehydrogenase
D-Lactate dehydrogenase, Microorganism (D-LDH) is an oxidoreductase enzyme that catalyzes the conversion of D-lactate to pyruvate, utilizing NAD+ or NADP+ as an electron acceptor. This enzyme is prevalent in various bacteria and fungi, making it a valuable tool in biochemical research. Applications include studies on metabolic pathways, fermentation processes, and the investigation of microbial physiology. -
Lactate Dehydrogenase Inhibitor
3-Acetylpyridine adenine dinucleotide is a potent inhibitor of lactate dehydrogenase (LDH), an enzyme critical for the conversion of pyruvate to lactate in cellular metabolism. As an analog of nicotinamide adenine dinucleotide (NAD), it offers valuable insight into NAD-dependent enzymatic processes. This compound is useful in both biochemical studies and metabolic research, providing a means to explore LDH's role in various pathophysiological conditions. -
Lactate Dehydrogenase Inhibitor
Glomeratose A is a potent lactate dehydrogenase inhibitor derived from the plant Polygala tenuifolia. This compound demonstrates significant biological activity by modulating lactate production, thereby impacting metabolic processes associated with various diseases. Research applications include investigations into metabolic pathways, cancer biology, and the role of lactate in cellular signaling. -
Lactate Dehydrogenase Inhibitor
LDHA-IN-5 is a potent inhibitor of lactate dehydrogenase (LDHA), targeting its enzymatic activity to modulate metabolic pathways. This compound exhibits significant potential in research applications related to metabolic disorders, including primary hyperoxaluria. By inhibiting LDHA, LDHA-IN-5 may help to reduce lactate levels and influence cellular metabolism, making it a valuable tool for understanding disease mechanisms and developing therapeutic strategies. -
PCSK9 Inhibitor
MeIm is a potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) that acts as a peptide mimetic. It effectively enhances the cellular uptake of low-density lipoprotein (LDL) with an EC50 value of 6.04 μM by disrupting the interaction between PCSK9 and LDL receptors (LDLR), with an IC50 of 11.2 μM. MeIm is valuable for research focused on cardiovascular diseases and related lipid metabolism studies. -
PCSK9 Inhibitor
BRD8518 is a potent inhibitor of PCSK9, exhibiting an EC50 of 0.23 μM. By upregulating LDLR expression, BRD8518 effectively lowers blood lipid levels and enhances LDL uptake. This compound is valuable for research applications focused on cardiovascular diseases, facilitating the exploration of lipid metabolism and associated therapeutic strategies. -
LXR Antagonist
PFM046 is a potent antagonist of the liver X receptors (LXRα and LXRβ), demonstrating IC50 values of 2.04 μM and 1.58 μM, respectively. This compound effectively inhibits the expression of stearoyl-CoA desaturase 1 (SCD1) and fatty acid synthase (FASN), while promoting the expression of ATP-binding cassette transporter A1 (ABCA1). PFM046 has shown promising antitumor efficacy in preclinical mouse models, making it a valuable tool for research in cancer therapeutics and lipid metabolism pathways. -
SREBP Maturation Inhibitor
4'-Hydroxyflavanone is an inhibitor of SREBP maturation, impacting lipid synthesis. As a synthetic analogue of flavanone, it demonstrates potential in studies related to hepatic steatosis and dyslipidemia. This compound can be utilized to explore mechanisms of lipid metabolism and associated disorders. -
SREBP/SCAP Inhibitor
SREBP/SCAP-IN-1 is a selective inhibitor of the SREBP/SCAP complex, which plays a crucial role in lipid metabolism and cellular cholesterol homeostasis. This compound effectively disrupts the signaling pathway involved in sterol regulatory element-binding protein activation, providing insight into lipid regulation mechanisms. Research applications include investigating metabolic disorders, cardiovascular diseases, and potential therapeutic strategies targeting cholesterol metabolism. -
SREBP/SCAP Inhibitor
SREBP/SCAP-IN-2 is a selective inhibitor of the SREBP/SCAP complex, which plays a crucial role in lipid metabolism and cellular cholesterol homeostasis. This compound effectively interferes with the activation and function of SREBP, thereby modulating lipid biosynthesis pathways. SREBP/SCAP-IN-2 is valuable for research focusing on metabolic disorders, obesity, and cardiovascular diseases, providing insights into the regulatory mechanisms of lipid metabolism. -
FXR agonist
Deoxycholic acid 3-O-β-D-glucuronide disodium is a potent agonist of the farnesoid X receptor (FXR). This compound has been shown to play a significant role in regulating bile acid homeostasis, lipid metabolism, and glucose metabolism. Its applications include the study of metabolic disorders, liver diseases, and potential therapeutic strategies targeting FXR signaling pathways. -
FXR Antagonist
Tauro-β-muricholic acid sodium is a competitive and reversible antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 of 40 μM. This compound plays a significant role in the modulation of bile acid signaling and is utilized in research applications related to metabolic diseases, liver function, and cholesterol homeostasis. Its ability to inhibit FXR makes it a valuable tool for studying the physiological and pathological roles of bile acids in various biological systems. -
FXR Agonist
FXR Agonist 3 is a potent farnesoid X receptor (FXR) agonist, designed for the treatment of non-alcoholic steatohepatitis (NASH). This compound effectively inhibits the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, showcasing significant anti-fibrogenic properties. Additionally, FXR Agonist 3 markedly reduces liver steatosis and inflammation while improving levels of liver fibrosis, making it a valuable tool in liver disease research. -
FXR Agonist
Arjungenin is a pentacyclic triterpenoid that serves as a potent agoinist of the farnesoid X receptor (FXR). It enhances insulin sensitivity by modulating the functionality of adipocytes, making it relevant for metabolic research. In addition, Arjungenin demonstrates moderate free radical scavenging activity and exhibits inhibitory effects on the growth of Spilarctia obliqua larvae. Its antiviral properties include significant activity against various viruses, notably chikungunya virus (CHIKV). -
FXR Activators
Chenodeoxycholic acid 3-glucuronide is an active metabolite of Chenodeoxycholic acid that serves as a selective Farnesoid X receptor (FXR) activator, exhibiting an EC50 of 8 μM in in vitro assays. This compound effectively modulates FXR signaling pathways, which are crucial for bile acid homeostasis and lipid metabolism. Research applications include studying metabolic disorders, liver physiology, and the potential therapeutic effects of FXR activation in various disease models. -
FXR Antagonist
FXR Antagonist 1 is a selective antagonist of the farnesoid X receptor (FXR) with an IC50 of 2.1 μM. This compound effectively inhibits intestinal FXR signaling, promoting feedback activation of hepatic FXR. Its primary biological activity involves ameliorating hepatic steatosis, inflammation, and fibrosis in models of nonalcoholic steatohepatitis (NASH). FXR Antagonist 1 is a valuable tool for research focused on NASH and related metabolic disorders. -
FXR Agonist
Omesdafexor is a potent FXR agonist characterized by its unique non-bile acid structure, demonstrating efficacy in modulating bile acid and lipid metabolism. This compound is particularly relevant for research in non-alcoholic steatohepatitis (NASH), offering insights into therapeutic strategies for metabolic liver diseases. Its oral bioactivity facilitates its application in in vivo studies, making it a valuable tool for investigating FXR-related pathways in liver health and disease. -
FXR Activator
Linafexor is a potent FXR ( Farnesoid X Receptor) agonist that modulates bile acid homeostasis. By activating FXR, it plays a crucial role in regulating liver function. This compound is particularly relevant for research on primary sclerosing cholangitis (PSC) and metabolic dysfunction-associated steatohepatitis (MASH), offering insights into therapeutic strategies for liver-related diseases. -
FXR/FABP1 Dual Modulator
ZLY28 is a first-in-class dual modulator targeting farnesoid X receptor (FXR) and fatty acid-binding protein 1 (FABP1). This orally active compound exhibits significant potential as an anti-NASH agent, making it a valuable tool for research into nonalcoholic steatohepatitis (NASH) and related metabolic conditions. Its intestinal-restricted activity highlights its specificity, providing an innovative approach to studying lipid metabolism and liver function. -
FXR Antagonist
V023-9340 is a potent antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 of 4.27 μM. This compound is a valuable tool for investigating the role of FXR in the pathology of nonalcoholic steatohepatitis (NASH) and other related metabolic disorders. Its inhibitory action allows for the exploration of FXR's involvement in lipid metabolism and inflammation pathways, making it useful in therapeutic research targeting these conditions. -
FXR Agonist
Glyco-Obeticholic acid is an active metabolite of Obeticholic acid and acts as a farnesoid X receptor (FXR) agonist. By activating FXR, it plays a vital role in regulating bile acid homeostasis, lipid metabolism, and glucose metabolism. This compound is primarily used in research to investigate metabolic disorders, liver diseases, and potential therapeutic strategies for cholestatic liver conditions. -
FXR Agonist
FXR Agonist 5 functions as a selective agonist for the farnesoid X receptor (FXR). This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research on metabolic disorders characterized by inflammation. Its application extends to studying the role of FXR in regulating bile acid homeostasis and glucose metabolism, thus providing insights into potential therapeutic strategies for related diseases. -
FXRα Antagonist
NDB is a selective antagonist of the human farnesoid X receptor alpha (hFXRα), serving to modulate the transcription of downstream genes associated with this pathway. This compound demonstrates potential in anti-diabetic research by influencing metabolic processes regulated by FXRα. Its application is particularly relevant for studies investigating the role of bile acids and metabolism in diabetes and related disorders. -
FXR Agonist
HEC96719 is a selective tricyclic agonist of the farnesoid X receptor (FXR) that demonstrates potent activity with EC50 values of 1.37 nM and 1.55 nM in time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. This compound has shown significant efficacy in improving non-alcoholic steatohepatitis (NASH) and liver fibrosis, exhibiting favorable distribution in liver and intestinal tissues. HEC96719 is valuable for research focusing on non-alcoholic steatohepatitis and related liver conditions. -
FXR Agonist
Cholic acid 3-O-glucuronide disodium is an agonist of the farnesoid X receptor (FXR), exhibiting an EC50 value of 91.5 μM. This compound plays a significant role in the study of bile acid metabolism and detoxification processes. It is a valuable reagent for research applications focused on liver function and metabolic regulation. -
FXR Agonist
FXR agonist 4 is an agonist of the farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. It demonstrates significant efficacy in ameliorating hyperlipidemia, hepatic steatosis, insulin resistance, and hepatic inflammation in dietary-induced obesity (DIO) mouse models. This compound is valuable for research focused on non-alcoholic fatty liver disease (NAFLD) and its associated metabolic disorders. -
FXR Antagonist
β-FXR antagonist 1 is a selective antagonist of the Farnesoid X receptor (FXR), a key regulator of bile acid and lipid metabolism. This compound has demonstrated biological activity in inhibiting FXR-mediated signaling pathways, making it valuable for research focused on metabolic diseases and liver function. Its application spans studies on cholesterol homeostasis, insulin sensitivity, and potential therapeutic interventions in conditions such as non-alcoholic fatty liver disease (NAFLD). -
FXR Agonist
BMS-986318 is a potent non-bile acid agonist of the farnesoid X receptor (FXR), exhibiting EC50 values of 53 nM and 350 nM in FXR Gal4 and SRC-1 recruitment assays, respectively. This compound possesses a favorable ADME profile and has demonstrated efficacy in preclinical models of liver cholestasis and fibrosis, particularly in mouse bile duct ligation studies. BMS-986318 is suitable for research related to nonalcoholic steatohepatitis and its potential therapeutic implications. -
FXR Activator
NR1H4 activator 1 is a highly selective agonist of the Farnesoid X Receptor (FXR), demonstrating exceptional FXR activation with an EC50 value of 1 nM in human assays. This compound has been identified for its potential therapeutic applications in gastrointestinal diseases. Its potent activity makes it a valuable tool for research focused on metabolic regulation and liver health. -
FXR Agonist
Danifexor is a selective agonist of the farnesoid X receptor (FXR), which plays a crucial role in regulating bile acid, lipid, and glucose metabolism. Its activation of FXR is associated with beneficial effects on metabolic disorders and liver diseases. Danifexor is utilized in research exploring therapeutic avenues for conditions such as non-alcoholic fatty liver disease (NAFLD) and hyperlipidemia. -
Fxr Agonist
Hedragonic acid is an oleane-type triterpenoid that acts as a potent agonist for the farnesoid X receptor (FXR). This compound has demonstrated protective effects against liver damage induced by acetaminophen overdose and is effective in reducing liver inflammation. Hedragonic acid is valuable for research focused on liver health, metabolic disorders, and the modulation of bile acid homeostasis.
