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Catalog No.
Product Name
Application
Product Information
Citations
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Fluorescently-tethered Hsp90 Inhibitor
HS-27 is a fluorescently-tethered inhibitor targeting Heat Shock Protein 90 (Hsp90), facilitating the assessment of surface Hsp90 expression on intact tissue specimens. Comprising core elements of SNX-5422 linked through a PEG spacer to a fluorescein derivative, HS-27 selectively binds to ectopically expressed Hsp90. This reagent is particularly valuable in breast cancer research, providing a tool for applications involving visualization and treatment strategies. -
Hsp27 Inhibitor
Apatorsen is a 2'-methoxyethyl-modified antisense oligonucleotide that functions as a Heat Shock Protein 27 (Hsp27) inhibitor. By reducing Hsp27 mRNA and protein levels, Apatorsen disrupts stress-induced cytoprotective mechanisms, promotes apoptosis, inhibits tumor growth, and prevents metastasis. This compound is particularly relevant for research focused on non-small cell lung cancer, castration-resistant prostate cancer, breast cancer, ovarian cancer, and bladder cancer. -
HSP90 Inhibitor
Aminohexylgeldanamycin (AHGDM) is a potent inhibitor of HSP90, a chaperone protein essential for the proper folding and function of many oncoproteins. This compound exhibits significant antiangiogenic and antitumor activities, making it a valuable tool in cancer research. Its ability to disrupt HSP90 function highlights its potential in the study of tumor biology and therapeutic interventions targeting heat shock proteins. -
HSP90 Inhibitor
CH5015765 is a potent HSP90 inhibitor that targets the N-terminal ATP binding site with a dissociation constant of 3.4 nM. This compound demonstrates significant antiproliferative activity, exhibiting IC50 values of 0.46 μM in HCT116 colorectal cancer cells and 0.57 μM in NCI-N87 gastric cancer cells. CH5015765 is suitable for research applications focused on cancer biology and therapeutic development. -
HSP90 Inhibitor
HSP90-IN-27 is a potent inhibitor of the heat shock protein 90 (HSP90), which plays a critical role in protein folding and stabilization of client proteins involved in cancer progression. This compound effectively disrupts HSP90 function, leading to the degradation of oncogenic proteins and subsequent inhibition of tumor growth. HSP90-IN-27 is applicable in cancer research, particularly in studies focused on targeted therapies and the molecular chaperone network. -
Hsp60-Hsp10 Inhibitor
[Au(TPP)]Cl is an inhibitor of the Hsp60-Hsp10 complex, which plays a critical role in protein folding and cellular stress responses. This compound demonstrates significant anticancer activity by disrupting the refolding process of misfolded proteins, thereby promoting cell apoptosis in cancerous cells. [Au(TPP)]Cl is valuable for research applications targeting cancer therapy and understanding the molecular mechanisms of chaperone functions. -
Hsp90 Inhibitor
Onalespib lactate is a highly potent inhibitor of heat shock protein 90 (Hsp90) with a Kd of 0.71 nM, demonstrating the capability to cross the blood-brain barrier. This compound effectively inhibits tumor cell proliferation, survival, and migration, while reducing the expression of key signaling proteins such as EGFR, p-EGFR, AKT, P-AKT, ERK1/2, P-ERK1/2, S6, and P-S6. With its significant antitumor activity, Onalespib lactate is particularly relevant for research into non-small cell lung cancer (NSCLC). -
HSP90 Inhibitor
HSP90-IN-11 is a potent inhibitor of HSP90, exhibiting strong inhibition of HSP90α activity. This compound demonstrates significant antiproliferative effects in colorectal cancer (CRC) and non-small cell lung cancer (NSCLC) cell lines, with IC50 values in the low double-digit nanomolar range. HSP90-IN-11 facilitates the rapid degradation of client proteins such as EGFR and Akt in NSCLC cells and induces a notable accumulation of sub-G1 phase cell populations, highlighting its potential for cancer research applications. -
Hsp90 inhibitor
BX-2819 is a potent inhibitor of Heat Shock Protein 90 (Hsp90) with an IC50 value of 41 nM. This compound effectively inhibits the proliferation of various cancer cell lines and has demonstrated significant antitumor activity in vivo, notably reducing the growth of NCI-N87 and HT-29 tumors in nude mouse models. BX-2819 is a valuable tool for research into cancer biology and potential therapeutic strategies targeting Hsp90. -
Hsp90a Inhibitor
CH5164840 is a potent inhibitor of the N-terminal domain of Hsp90a, exhibiting a high binding affinity with a Kd value of 0.52 nM. This compound demonstrates significant anti-proliferative effects against various human cancer cell lines, including HCT116 and NCI-N87, with IC50 values of 0.15 μM and 0.066 μM, respectively. Additionally, CH5164840 has an oral bioavailability profile with a half-life of 2.64 hours, indicating its potential for effective antitumor applications in therapeutic settings. -
Hsp90 Inhibitor
HSP90-IN-19 is a potent inhibitor of heat shock protein 90 (Hsp90), identified for its effective inhibitory activity with an IC50 value of 0.27 μM. This compound is relevant for studies investigating viral infections, neurodegenerative diseases, and inflammatory processes. Its ability to modulate cellular stress response pathways makes it a valuable tool in biochemical research and drug development efforts targeting Hsp90. -
PDE5 Inhibitor
Amino Tadalafil is an inhibitor of phosphodiesterase type 5 (PDE5), acting similarly to its structural analog, tadalafil. It exhibits a significant cross-reactivity of 105.2% with anti-tadalafil polyclonal antibodies, enabling specific detection in various assays. Due to its properties, Amino Tadalafil is suitable for incorporation into dietary supplements and offers potential applications in research exploring erectile dysfunction and cardiovascular health. -
HMG-CoA Inhibitor
(3R,5R)-Rosuvastatin Lactone is an HMG-CoA reductase inhibitor that plays a crucial role in cholesterol biosynthesis modification. This compound exhibits potent lipid-lowering effects, making it valuable for studying dyslipidemia and related cardiovascular diseases. Its applications extend to elucidating mechanisms of action in statin therapies and examining its impact on metabolic pathways. -
NNMT Inhibitor
NNMT-IN-4 is a selective and uncompetitive inhibitor of nicotinamide N-methyltransferase (NNMT) with demonstrated membrane permeability. It exhibits IC50 values of 42 nM in biochemical assays and 38 nM in cell-based assays, indicating potent inhibition. With favorable pharmacokinetic and pharmacodynamic profiles, along with excellent oral bioavailability, NNMT-IN-4 serves as a valuable in vivo chemical probe for NNMT research applications. -
α-Glucosidase Inhibitor
Rebaudioside A is an α-glucosidase inhibitor that demonstrates an IC50 value of 35.01 μg/mL. This steviol glycoside enhances insulin secretion in pancreatic β cells through a glucose-dependent mechanism, which involves the inhibition of KATP channels and subsequent depolarization and calcium influx. Additionally, Rebaudioside A regulates cholesterol metabolism by activating the SREBP signaling pathway and inhibiting HMGCR, leading to increased LDL receptor expression. It is suitable for research in the areas of blood glucose and lipid regulation, as well as obesity management. -
MAO Inhibitor
Rosmarinic acid racemate acts as a monoamine oxidase inhibitor, specifically targeting the MAO-A and MAO-B enzymes as well as catechol-O-methyltransferase (COMT). It demonstrates inhibition with IC50 values of 50.1 μM for MAO-A, 184.6 μM for MAO-B, and 26.7 μM for COMT. This compound is useful in research applications focused on neurochemical regulation, mood disorders, and the modulation of catecholamine levels. -
CYP1A Inhibitor
Dibenzothiophene is a noncompetitive inhibitor of cytochrome P450 1A (CYP1A), effectively inhibiting CYP1A-mediated ethoxyresorufin O-deethylation (EROD) activity with a Km value of 0.592 μM. This compound interacts with the aryl hydrocarbon receptor (AHR) pathway and has been shown to enhance the embryotoxicity of β-naphthoflavone. Its acute toxicity in animal models underscores its relevance in research. Dibenzothiophene is primarily utilized in studies investigating the mechanisms of developmental toxicity in various organisms. -
Endogenous Metabolite,Cancer Inhibitor
Protoporphyrin IX is an endogenous metabolite and a potent cancer inhibitor, functioning primarily as a radiation sensitizer. It enhances reactive oxygen species (ROS) generation, even under hypoxic conditions, leading to increased DNA damage. As a photosensitizer, Protoporphyrin IX undergoes photobleaching upon light exposure, facilitating targeted cancer therapies. Research indicates its efficacy in treating basal cell carcinoma and offers promise for sonodynamic and photodynamic applications in various cancers, including bladder cancer. -
Bacterial Inhibitor
Ceftezole is a broad-spectrum cephem antibiotic that effectively targets both gram-positive and gram-negative bacteria. Its primary mechanism involves inhibiting bacterial cell wall synthesis, making it valuable in combating various bacterial infections. Additionally, Ceftezole acts as an alpha-glucosidase inhibitor, demonstrating potential in in vivo anti-diabetic applications. It is suitable for use in microbiological research and studies related to diabetes management. -
Bacterial Inhibitor
Ceftezole sodium is a broad-spectrum cephem antibiotic primarily targeting various gram-positive and gram-negative bacteria. Its mechanism of action involves inhibiting bacterial cell wall synthesis, leading to cell lysis and death. Additionally, ceftezole sodium demonstrates alpha-glucosidase inhibition, contributing to its in vivo anti-diabetic effects. This compound is relevant for research in microbial resistance and diabetes therapeutic development. -
Mutant IDH2 Inhibitor
Enasidenib mesylate is a selective inhibitor of mutant isocitrate dehydrogenase 2 (IDH2) enzymes, demonstrating potent and reversible binding. It primarily exerts its biological activity by altering the metabolism of 2-hydroxyglutarate, thus affecting cellular processes associated with cancer progression. This compound is utilized in research focused on hematologic malignancies, particularly those driven by IDH2 mutations. -
DHFR Inhibitor
Proguanil is a potent dihydrofolate reductase (DHFR) inhibitor, primarily utilized in antimalarial research. Upon administration, it is metabolized to Cycloguanil, its active form, enhancing its efficacy against Plasmodium species. This compound is essential for studying the biochemical pathways of folate metabolism and developing therapeutic strategies against malaria. -
Monoamine Oxidase Inhibitor
Pheniprazine hydrochloride is a potent monoamine oxidase inhibitor that plays a significant role in modulating neurotransmitter levels. This compound is primarily utilized in depression research, offering insights into the biochemical pathways associated with mood regulation. Its long-acting properties make it a valuable reagent for studies investigating monoamine metabolism and related neuropsychological disorders. -
α-glucosidase/α-amylase Inhibitor
2-Hydroxyquinoline is a selective inhibitor of α-glucosidase and α-amylase, exhibiting IC50 values of 64.4 µg/mL and 130.5 µg/mL, respectively. This compound is valuable for investigating carbohydrate metabolism and can be utilized in research related to diabetes management and treatment strategies. Its inhibitory effects contribute to a deeper understanding of enzymatic roles in glucose absorption and metabolism. -
Ferroptosis Inhibitor
Isoeugenol acetate is a ferroptosis inhibitor derived from isoeugenol. This compound has been shown to modulate cell death mechanisms associated with oxidative stress, making it a valuable tool for investigating ferroptosis in various biological contexts. Its applications extend to research in cancer biology, neurodegenerative diseases, and other conditions where ferroptosis plays a critical role. -
IDO1 Inhibitor
2-Hydrazinobenzothiazole is a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), exhibiting an IC50 of 8 μM. This compound targets the heme group of IDO1 via hydrazine interactions, thereby modulating immune responses. It is primarily utilized in research related to immune system disorders and therapeutic interventions aimed at enhancing immune function. -
α-glucosidase Inhibitor
3,4-Methylenedioxychalcone is an α-glucosidase inhibitor with a reported IC50 of 1870 μM. This compound is relevant for research applications focused on type 2 diabetes, as it may help modulate carbohydrate metabolism by delaying the breakdown of complex carbohydrates. Its potential to influence glucose absorption can be valuable for studies aimed at understanding and treating metabolic disorders. -
Monoamine Oxidase Inhibitor
Nialamide is a non-selective inhibitor of monoamine oxidase (MAO), playing a critical role in regulating reactive oxygen species (ROS) production. This compound has been shown to induce hyperkinesis in animal models, enhance the anticonvulsant effects of Diphenylhydantoin in mice, increase rectal temperature, and potentiate the pressor response to Norepinephrine. Nialamide is valuable for research related to depression, inflammatory diseases, neurodegenerative disorders, and hypertension. -
SGK1 Inhibitor
SGK1-IN-9 is an inhibitor of serum/glucocorticoid-regulated kinase 1 (SGK1). This compound exhibits potential anti-cancer activity by modulating cell survival pathways and influencing tumor cell proliferation. It is suitable for use in cancer research to investigate the role of SGK1 in various malignancies and explore therapeutic strategies targeting this kinase. -
Aromatase/CYP19 Inhibitor
(±) Homoeriodictyol is a potent inhibitor of aromatase (CYP19), an enzyme critical in estrogen biosynthesis. This compound is primarily utilized in breast cancer research to investigate estrogen-mediated pathways and their role in tumor growth. Its inhibitory activity makes it a valuable tool for studying therapeutic strategies targeting aromatase in hormone-related cancers. -
SGK1 Inhibitor
SGK1-IN-7 is a selective inhibitor of SGK1, exhibiting a blood-brain barrier permeability with an IC50 of 0.72 μM. This compound effectively reduces the phosphorylation of TAU protein at the Ser396 and Ser214 sites and counters the toxicity induced by Okadaic acid. SGK1-IN-7 is a valuable tool for research into the mechanisms underlying Alzheimer's disease. -
SGK1/GSK3β Inhibitor
SGK1-IN-8 is a potent inhibitor of SGK1 and GSK3β, exhibiting an IC50 of 0.11 μM against human SGK1 and 3.39 μM against human GSK3β. This compound effectively inhibits the catalytic activities of both SGK1 and GSK3β, leading to a reduction in the phosphorylation of the TAU protein at the Ser214 site. SGK1-IN-8 is utilized in research focused on Alzheimer's disease and related neurodegenerative disorders. -
Cathepsin Inhibitor
Cathepsin-IN-5 is a selective inhibitor of cathepsins L and S, exhibiting IC50 values of 6.2 μM and 81 nM, respectively. This compound effectively inhibits cancer cell proliferation and induces apoptosis, while also reducing the growth of hepatocellular tumors in mouse models. Additionally, Cathepsin-IN-5 modulates the expression of genes associated with cell death and proliferation, making it a valuable reagent for research into hepatocellular carcinoma. -
Hsp90 Inhibitor
Hsp90-IN-47 is a potent Hsp90 inhibitor, demonstrating an IC50 of 0.014 μM against Hsp90α. This compound exhibits significant antifungal properties, particularly when used in combination with Fluconazole, enhancing efficacy against fluconazole-resistant strains of Candida albicans. Additionally, Hsp90-IN-47 shows promising antitumor activity, particularly in acute myeloid leukemia and non-small cell lung cancer research applications. -
HO-1 Inhibitor
OB-24 free base is a selective inhibitor of heme oxygenase 1 (HO-1), demonstrating notable potential for targeting advanced prostate cancer. This compound effectively reduces protein carbonylation and diminishes the formation of reactive oxygen species in prostate cancer cells through its specific inhibition of HO-1 activity. In vitro studies reveal that OB-24 significantly impairs cell proliferation, while in vivo experiments show a marked reduction in tumor growth and metastasis to lymph nodes and lungs. Additionally, OB-24 displays enhanced efficacy when used in conjunction with Taxol, making it a valuable tool for cancer research. -
Heme Oxygenase/Lanosterol 14α-Demethylase Inhibitor
Azalanstat dihydrochloride is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, demonstrating selective inhibitory activity against HO-1 (IC50 = 5.5 µM) and HO-2 (IC50 = 24.5 µM). This compound has been shown to reduce the maturation rate of rat oocytes and increase oocyte degeneration, as well as partially inhibit progesterone production in preovulatory follicles in rats. Its usage is pertinent in studies focused on reproductive biology and the biochemical pathways involving heme oxygenase and steroidogenesis. -
ubiquitin activating enzyme E1 Inhibitor
N,N-dimethyldithiocarbamate potassium is an inhibitor of the ubiquitin-activating enzyme E1, leading to a decrease in the levels of activated ubiquitinated E1 (ub-E1). This compound is known to elevate intracellular copper levels, enhance oxidative stress, raise protein carbonyl levels, and promote the expression of heme oxygenase-1 (HO-1). N,N-dimethyldithiocarbamate potassium is particularly relevant for research into neurodegenerative disorders, including Parkinson's disease, by elucidating the impact of ubiquitin pathways on cellular stress responses. -
Monoamine Oxidase Inhibitor
Pheniprazine is a potent monoamine oxidase inhibitor that demonstrates a long-lasting effect on neurotransmitter levels. It is primarily utilized in research focused on the mechanisms underlying depression and other mood disorders. By inhibiting the breakdown of monoamines, Pheniprazine enhances mood-regulating neurotransmitter availability, making it a useful tool for studying the neurochemical basis of depression. -
Alcohol Dehydrogenase Inhibitor
Camelliquercetiside D is a natural product that acts as an alcohol dehydrogenase inhibitor, demonstrating an IC50 of 41.5 μM against yeast ADH. This compound is isolated from the leaves of Camellia sinensis and exhibits notable scavenging activity against DPPH, making it valuable for research applications in enzymology and oxidative stress studies. -
Alcohol Dehydrogenase Inhibitor
Camelliquercetiside B is a natural product that serves as an alcohol dehydrogenase inhibitor. Isolated from the leaves of Camellia sinensis, it demonstrates significant inhibitory activity with an IC50 value of 13.7 μM against yeast alcohol dehydrogenase. In addition, Camelliquercetiside B displays scavenging activity against DPPH free radicals, making it a valuable tool for research in alcohol metabolism and oxidative stress studies. -
NNMT Inhibitor
LL320 is a selective inhibitor of Nicotinamide N-methyltransferase (NNMT), with an apparent Ki of 6.8 nM. This compound has demonstrated interactions with RNA N-methyltransferase (RNMT), diphthamide biosynthesis 5 (DPH5), and S-adenosylhomocysteine hydrolase (SAHH). LL320 is valuable for research applications focused on metabolic regulation, cancer biology, and the exploration of NNMT-related pathways. -
FASN inhibitor
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression.
