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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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 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. -
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. -
CES2 inhibitor; FXR agonist;
FXR/CES2 modulator 1 is a dual modulator that functions as an FXR agonist and a CES2 inhibitor. This compound demonstrates significant potential in reducing the intestinal toxicity associated with irinotecan administration. Its unique mechanism of action makes it a valuable tool for research aimed at understanding FXR modulation and its implications in gastrointestinal safety during chemotherapy. -
ER α-glucosidases Inhibitor
IHVR-11029 is a potent small molecule inhibitor of ER α-glucosidases, demonstrating an EC50 of 0.09 μM. This compound is primarily utilized in research for exploring glucosidase enzymatic activity and its implications in metabolic disorders. Its specificity and efficacy make it a valuable tool for studies investigating glycosylation processes and related pathways. -
α-glucosidase Inhibitor
CM-10-18 is a potent inhibitor of α-glucosidases I and II, demonstrating significant activity in vitro and in animal models. This compound also exhibits antiviral properties by inhibiting dengue virus (DENV) infection in cultured human cells, while effectively reducing peak viremia in mice. CM-10-18 is valuable for research applications related to glycosidase inhibition and viral pathogenesis. -
α-Glucosidase Inhibitor
α-Glucosidase-IN-5 is a potent α-glucosidase inhibitor, exhibiting an IC50 of 57.9 µM. This compound is valuable for studying the modulation of carbohydrate metabolism and has potential applications in diabetes mellitus research. By inhibiting α-glucosidase, α-Glucosidase-IN-5 may aid in the investigation of glycemic control and the development of therapeutic strategies for diabetes management. -
α-glucosidase Inhibitor
Gallacetophenone is a potent inhibitor of α-glucosidase, displaying an IC50 value of 408.6 μM. This compound demonstrates synergistic effects on mammalian α-glucosidase when combined with 1-Deoxynojirimycin at elevated concentrations. Gallacetophenone is valuable for research into metabolic disorders, particularly type 2 diabetes, by facilitating the understanding of carbohydrate metabolism and its implications in glycemic control. -
α/β-Glucosidases Inhibitor
Castanospermine is a natural alkaloid primarily recognized for its role as an α/β-glucosidase inhibitor. This compound exhibits significant biological activities, including anti-inflammatory and antiviral properties, as well as the potential to impede metastatic progression in prostate cancer. Additionally, Castanospermine has applications as an immunosuppressant, proving useful in preventing transplant rejection. Its diverse functionalities make it a valuable tool in various areas of biochemical research. -
β-Hexosaminidase Inhibitor
M-31850 is a selective and competitive inhibitor of β-hexosaminidase, demonstrating IC50 values of 6.0 μM for human HexA and 3.1 μM for human HexB. This compound also inhibits β-N-acetyl-D-hexosaminidase (OfHex2) with a Ki of 2.5 μM. M-31850 is valuable for research applications focused on lysosomal storage disorders and other biological contexts where β-hexosaminidase activity is implicated. -
α-glucosidase I Inhibitor
Kojibiose is an α-glucosidase I inhibitor that functions as an orally active prebiotic disaccharide. It specifically inhibits the activity of α-glucosidase I, promoting the proliferation of beneficial gut bacteria such as Bifidobacterium and lactic acid bacteria. Additionally, kojibiose serves as a low-calorie sweetener that enhances iron absorption and exhibits antitoxic properties. In vivo studies demonstrate its ability to reduce hepatic expression of inflammatory markers, highlighting its potential applications in metabolic and gastrointestinal research. -
ColA Inhibitor
4',5-Dihydroxyflavone is a potent inhibitor of collagenase A (ColA), with an IC50 value of less than 1 μM. This flavonoid compound also shows inhibitory activity against α-glucosidase and soybean lipoxygenase-1, making it valuable in biochemical research. Its applications include studies focused on anti-toxicity and anti-diabetes, highlighting its potential therapeutic benefits in metabolic and inflammatory disorders. -
α-L-fucosidase Inhibitor
Deoxyfuconojirimycin hydrochloride is a selective inhibitor of α-L-fucosidase, demonstrating a Ki value of 10 nM for human liver lysosomal α-L-fucosidase and 140 nM for Charonia lampas α-L-fucosidase. This compound effectively inhibits the activity of all soluble α-L-fucosidases present in human liver, including various post-translationally modified enzyme forms. Deoxyfuconojirimycin hydrochloride is primarily utilized in research focused on fucosidase-related enzyme activity and metabolic pathways, though it does not exhibit anti-HIV properties. -
Tyrosinase Inhibitor
Kushenol A, a non-competitive inhibitor of tyrosinase, effectively blocks the conversion of L-tyrosine to L-DOPA, with IC50 and Ki values of 1.1 μM and 0.4 μM, respectively. Isolated from the root of Sophora flavescens, Kushenol A exhibits antioxidant properties and also inhibits alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. This compound is valuable for research focused on skin whitening and anti-aging applications due to its enzyme inhibitory effects. -
Glucosidase Inhibitor
Gitogenin is a natural steroid derived from the plant Tribulus longipetalus, serving as a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and α-glucosidase. It exhibits an IC50 of 0.69 μM for UGT1A4 using trifluoperazine as a substrate, and an IC50 of 37.2 μM for α-glucosidase. Gitogenin does not interfere with the activities of major human cytochrome P450 isoforms, making it a valuable reagent for studies in metabolic enzyme pathways and potential therapeutic applications related to glycemic control. -
Glycosidase Inhibitor
Cedryl acetate is a tricyclic sesquiterpene with notable α-glucosidase inhibitory activity. This compound is isolated from the plant Cunninghamia lanceolata and is valuable in research focused on carbohydrate metabolism and glycosidase inhibition. Its biological activity makes it an important tool for studying metabolic disorders and potential therapeutic interventions. -
GCase 2 Inhibitor
AMP-Deoxynojirimycin is a potent inhibitor of glucocerebrosidase 2 (GCase 2) and ceramide glucosyltransferase. This compound effectively interferes with glucosylceramide (GlcCer) biosynthesis, making it valuable for research related to lysosomal storage disorders and sphingolipid metabolism. Its biological activity positions AMP-Deoxynojirimycin as a significant tool for investigating the roles of GlcCer in various cellular processes and disease mechanisms. -
Glucosidase Inhibitor
Kaempferol 3-O-gentiobioside is a flavonoid that functions as an α-glucosidase inhibitor. Isolated from the leaves of C. alata, this compound demonstrates significant antidiabetic activity by inhibiting carbohydrate enzyme activity, with an IC50 value of 50.0 µM. It serves as a valuable tool for research into glucose metabolism and diabetes treatment applications. -
Glycosidase Inhibitor
Glycyrrhisoflavone is a potent α-glucosidase inhibitor that acts primarily by blocking the enzyme's activity, thereby modulating carbohydrate metabolism. This natural prenylflavonoid exhibits significant biological activity, making it useful in research related to diabetes management and metabolic disorders. Its ability to influence glycemic control highlights its potential applications in pharmacological studies and nutraceutical development. -
Weed Inhibitor
Glucobrassicin potassium is a glucosinolate (GSL) that functions as a potent weed inhibitor. Isolated from wild carrot (Raphanus raphanistrum L.), it demonstrates significant potential in biological fumigation and allelopathy research. Its application in weed management studies supports the exploration of sustainable agricultural practices. -
GCase Inhibitor
Gcase Activator 2 is a pyrrolo[2,3-b]pyrazine that serves as a potent activator of β-glucocerebrosidase (GCase), with an EC50 of 3.8 μM. This compound facilitates GCase dimerization, promoting both K-type and V-type interactions. Gcase Activator 2 displays low metabolic clearance in both human and mouse systems, making it a valuable tool for research into GCase-related biological pathways and potential therapeutic applications in lysosomal storage disorders. -
CHI3L1 Inhibitor
CHI3L1-IN-3 is a potent inhibitor of CHI3L1, with dissociation constants of 13.76 μM and 13.5 μM as measured by MST and SPR assays, respectively. This compound exhibits favorable pharmacokinetic properties, including extended plasma half-lives and microsomal stability, alongside decreased intrinsic clearance. In biological assays, CHI3L1-IN-3 demonstrates dose-dependent cytotoxicity, effectively reduces spheroid mass, and inhibits cell migration in a three-dimensional multicellular glioblastoma (GBM) spheroid model. It serves as a valuable tool for investigating the roles of CHI3L1 in GBM research. -
Alpha-glucosidase Inhibitor
Valiolamine is an aminocyclitol that functions as an alpha-glucosidase inhibitor. It exhibits significant inhibitory activity against porcine intestinal sucrase and maltase, with Ki values of 30 nM and 350 nM, respectively. This compound is valuable for research applications focused on carbohydrate metabolism, specifically in studying the modulation of glucose absorption and the potential therapeutic approaches to disorders such as diabetes. -
α-Glucosidase Inhibitor
Panasenoside is a flavonoid that acts as an α-glucosidase inhibitor. Derived from Lilium pumilum DC, it has demonstrated significant inhibitory activity against α-glucosidase, making it a valuable tool for research on carbohydrate metabolism and related disorders. This compound is relevant for studies investigating diabetes management and the modulation of postprandial blood glucose levels. -
CHI3L1:HSIII Inhibitor
CHI3L1-IN-2 is a selective inhibitor of CHI3L1 (Chitinase-3-Like Protein 1) that targets its interaction with heparan sulfate (CHI3L1:HSIII), exhibiting an IC50 of 26 nM. CHI3L1 is a glycoprotein linked to various pathological conditions including inflammation, fibrosis, and cancer. This compound serves as a valuable tool for researchers investigating the role of CHI3L1 in disease processes and therapeutic applications. -
α-Glucosidase Inhibitor
β-Hydroxypropiovanillone is an α-glucosidase inhibitor that demonstrates significant concentration-dependent inhibitory effects on this enzyme. With an IC50 value of 257.8 μg/mL, it is useful for studying carbohydrate metabolism and potential therapeutic applications in managing postprandial hyperglycemia. This compound may serve as a valuable research tool in the exploration of diabetes and related metabolic disorders. -
α-glucosidase Inhibitor
Magnoloside B is an α-glucosidase inhibitor with an IC50 value of 0.69 mM, derived from the stem bark of Magnolia officinalis. It exhibits moderate inhibitory activity against MGC-803 and HepG2 cancer cell lines. This compound is of significant interest for research applications related to cancer and diabetes. -
α-amylase/α-glucosidase/Acetylcholinesterase Inhibitor
Kaempferol-3,7-di-O-β-glucoside is a flavonol that acts as an inhibitor of α-amylase, α-glucosidase, and acetylcholinesterase. This compound has demonstrated protective effects on differentiating neuronal cells, specifically SH-SY5Y, against injury induced by Amyloid β peptide. Its enzyme inhibitory properties and neuroprotective effects indicate potential applications in Alzheimer's disease research and therapeutics. -
Alpha-glucosidase Inhibitor
(+)-Afzelechin is an alpha-glucosidase inhibitor derived from the rhizomes of Bergenia ligulata. It demonstrates an ID50 value of 0.13 mM, indicating its potency in inhibiting alpha-glucosidase activity. This compound effectively delays carbohydrate absorption, thereby reducing postprandial hyperglycemia and hyperinsulinemia. It serves as a valuable tool for research in metabolic disorders and glycemic control. -
α-glucosidase Inhibitor
Ganoderol B is a potent inhibitor of α-glucosidase, exhibiting significant enzymatic inhibition with an IC50 value of 48.5 μg/mL (119.8 μM). This compound is primarily utilized in research applications related to carbohydrate metabolism and glucose regulation, making it a valuable tool in studies of diabetes and postprandial hyperglycemia. Researchers may leverage Ganoderol B to explore mechanisms of glycemic control and to develop therapeutic strategies targeting α-glucosidase. -
α-Glucosidase Inhibitor
(-)-Pinoresinol 4-O-glucoside serves as a potent α-glucosidase inhibitor, exhibiting an IC50 value of 48.13 µM. This compound promotes cell migration and early differentiation of pre-osteoblasts while enhancing the protein levels of BMP2, phosphorylated Smad1/5/8, and RUNX2. Additionally, it demonstrates protective effects against oxidative stress, hyperglycemia, and hepatic toxicity. (-)-Pinoresinol 4-O-glucoside is a valuable reagent for investigating osteoporosis and periodontal disease. -
GCase Inhibitor
Glucocerebrosidase-IN-1 is a selective inhibitor of glucocerebrosidase (GCase), exhibiting an IC50 of 29.3 μM and a Ki of 18.5 μM. This compound is instrumental in research related to Gaucher disease and Parkinson's disease, allowing for the investigation of GCase's role in these conditions. Its potency and specificity make it a valuable tool for elucidating the biochemical pathways involved in lysosomal storage disorders. -
α-Glucosidase Inhibitor (AGI)
α-Glucosidase-IN-11 is a potent competitive inhibitor of α-glucosidase, exhibiting an IC50 value of 0.56 μM. This compound selectively binds to tryptophan residues in the enzyme, influencing its protein folding and activity. α-Glucosidase-IN-11 has potential applications in the regulation of carbohydrate metabolism and blood glucose control, making it a valuable tool for diabetes research and therapeutic development. -
Glycosidase Inhibitor
N-Methylmoranoline is a potent α-glucosidase inhibitor that modulates carbohydrate metabolism by interfering with enzyme activity. This compound demonstrates significant potential in research related to diabetes management and metabolic disorders by reducing glucose absorption. It is utilized in studies exploring glycemic control and the pharmacological effects of glycosidase inhibition.
