Catalog No.
Product Name
Application
Product Information
Citations
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CYP1B1 Inhibitor
CYP1B1-IN-9 is a highly selective competitive inhibitor of CYP1B1, demonstrating an IC50 of 1.48 nM. It effectively inhibits the migration and invasion of A549/T cells and has been shown to resensitize cells resistant to Paclitaxel. Notable for its favorable pharmacokinetic properties, metabolic stability, and safety profile, CYP1B1-IN-9 serves as a valuable tool for investigating tumor-drug resistance mechanisms in cancer research. -
CYP2A6/MAO Inhibitor
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate functions as an irreversible inhibitor of CYP2A6, exhibiting IC50 values of 8.64 μM and 22.3 μM under pre-incubation and co-incubation conditions, respectively. Additionally, this compound demonstrates inhibitory activity against monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B), with IC50 values of 60.2 μM and 38.6 μM, respectively. It serves as a valuable tool for research involving drug metabolism, neurochemistry, and the study of pharmacological responses influenced by these metabolic pathways. -
Drug Metabolite
3-Hydroxyflunitrazepam is the principal metabolite of Flunitrazepam, formed through 3-hydroxylation by the enzyme CYP3A4. This metabolite constitutes over 80% of Flunitrazepam's metabolic pathway in liver microsomes, highlighting its relevance in pharmacokinetics. The formation of 3-Hydroxyflunitrazepam is significantly inhibited by CYP3A4 inhibitors such as Ketoconazole and Ritonavir, suggesting crucial implications for drug-drug interactions in therapeutic applications and metabolic studies. -
CYP2C9/CYP3A4 Inhibitor
GW694481 is a selective inhibitor of CYP2C9 and CYP3A4, exhibiting IC50 values of 2.1 μM and 17.0 μM, respectively. This compound functions as an ApoA1 upregulator, enhancing the expression of ApoA1 in human hepatic cells. GW694481 is valuable for research focused on atherosclerosis and related metabolic disorders, providing insights into lipid metabolism and cardiovascular health. -
RARβ/RARα Antagonist
LE135 is a selective antagonist of retinoic acid receptors RARα and RARβ, exhibiting a Ki of 1.4 μM for RARα and a significantly higher affinity of 220 nM for RARβ. This compound demonstrates high specificity for these targets, with minimal interaction with RARγ and RXR isoforms. Additionally, LE135 acts as a potent activator of TRPV1 and TRPA1 receptors, with EC50 values of 2.5 μM and 20 μM, respectively, making it a valuable tool for studying pathways involving these ion channels in various biological contexts. -
Drug Metabolite
Beclomethasone 17-propionate is a potent glucocorticoid receptor (GR) agonist and an active metabolite of Beclomethasone dipropionate. It demonstrates a higher affinity for the GR, making it more effective in modulating glucocorticoid activity. This compound effectively suppresses cytokine production in lung macrophages associated with chronic obstructive pulmonary disease (COPD), making it valuable for research in inflammation and respiratory disorders. -
11β-HSD1 Inhibitor
INCB13739 is a selective and potent inhibitor of 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1), exhibiting an IC50 of 3.2 nM in enzymatic assays and 1.1 nM in peripheral blood mononuclear cells (PBMC). This compound demonstrates significant potential for research in type 2 diabetes mellitus (T2DM) and obesity, targeting the regulation of glucocorticoid metabolism, which plays a critical role in metabolic conditions. Its tissue-specific action makes it a valuable tool for understanding 11β-HSD1-related pathways in metabolic disorders. -
Cyclic Di-nucleotide
2'2'-cGAMP is a synthetic cyclic dinucleotide (CDN) that targets the STING (Stimulator of Interferon Genes) pathway, playing a crucial role in the immune response. It effectively induces the production of interferon-beta (IFN-β), a key cytokine involved in antiviral defense. While 2'2'-cGAMP exhibits a weaker affinity for STING compared to 2'3'-cGAMP, it demonstrates a stronger interaction than other CDNs, making it valuable for research in immunology and therapeutic applications related to immune modulation. -
Fas receptor Antagonist
Xelafaslatide is a Fas receptor antagonist that effectively inhibits Fas receptor signaling, thereby blocking downstream apoptosis and inflammatory pathways. This compound demonstrates significant potential in suppressing neuroinflammation and microglial activation in glaucoma models, offering protection to retinal ganglion cells and preventing axonal degeneration. Xelafaslatide is relevant for research focused on glaucoma and related neurodegenerative conditions. -
Ser/Thr Protease Activator
Plasma kallikrein-IN-1 is a highly potent inhibitor of plasma kallikrein, exhibiting an IC50 of 0.5 nM. This compound selectively targets serine/threonine proteases, thereby modulating proteolytic pathways. It is primarily utilized in research exploring the roles of kallikrein in cardiovascular and inflammatory disorders. This compound is invaluable for studies aimed at understanding the therapeutic potential of kallikrein inhibition. -
Factor Xa Inhibitor
DPC423 free base is a selectively potent Factor Xa inhibitor, demonstrating inhibition constants (Kis) of 0.15 nM in humans and 0.3 nM in rabbits. It exhibits moderate selectivity with Kis of 60 nM against human trypsin, 61 nM against plasma kallikrein, and 6000 nM against thrombin. By inhibiting the formation of the prothrombinase complex, DPC423 reduces thrombin generation, thereby obstructing fibrin formation and platelet activation. This compound is valuable for research applications related to anticoagulation in arterial thrombosis. -
Kallikrein
Ono 3307 free base is a synthetic protease inhibitor that targets kallikrein and other serine proteases. It demonstrates protective effects against acute pancreatitis by inhibiting hyperamylasemia and pancreatic edema, while also reducing cathepsin B leakage from lysosomes in a dose-dependent manner. This compound has significant applications in research related to protease regulation and pancreatic function, making it valuable for studies exploring the pathophysiology of acute pancreatitis and related conditions. -
Somatostatin Receptor Antagonist
Cyclosomatostatin is a potent somatostatin receptor antagonist that specifically targets somatostatin receptor type 1 (SSTR1). This compound effectively inhibits SSTR1 signaling, leading to reduced cell proliferation, decreased ALDH+ cell population size, and diminished sphere formation in colorectal cancer cells. It serves as a valuable tool for research applications focused on understanding the role of somatostatin signaling in cancer biology. -
Somatostatin (1-28) Derivative
[Nle8] Somatostatin (1-28) is a derivative of somatostatin (1-28) in which norleucine substitutes for methionine at position 8. This compound enhances amylase release and elevates cyclic AMP levels in pancreatic acini. It is utilized in research to study pancreatic function and the regulatory mechanisms of peptide hormones in metabolic processes. -
Heme Oxygenase Inhibitor
Zn(II) Deuteroporphyrin IX 2,4 bis ethylene glycol is a potent inhibitor of heme oxygenase (HO), a key enzyme involved in the degradation of heme to bilirubin. By inhibiting HO activity, this compound can effectively reduce the release of hypothalamic hormones such as arginine vasopressin (AVP), oxytocin (OT), and atrial natriuretic peptide (ANP) under hyperosmotic conditions. Its application extends to research involving hyperbilirubinemia and the physiological implications of HO modulation. -
12-Lipoxygenase Metabolite
12(S)-HPETE, a metabolite of 12-lipoxygenase, plays a crucial role in regulating vascular tone. It induces the expression of c-Fos and c-Jun proteins while increasing activating protein 1 (AP-1) activity in vascular smooth muscle cells. This compound may be pivotal in vasomotor regulation, influencing interactions between endothelial cells and adjacent blood cells. 12(S)-HPETE is useful for investigating cerebrovascular tension in various research contexts. -
AhR Agonist
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist that binds directly to AhR, leading to the upregulation of key target genes such as CYP1A1, CYP1B1, and TIPARP. This compound demonstrates notable cell growth inhibitory effects and induces apoptosis specifically in triple-negative breast cancer cells. Its anti-tumor properties make ZSTK3744 a valuable tool for investigating mechanisms underlying chemoresistance in triple-negative breast cancer. -
AHR Inhibitor
IK-175 is a selective aryl hydrocarbon receptor (AHR) inhibitor that prevents the translocation of AHR from the cytoplasm to the nucleus. This compound exhibits high specificity for AHR, distinguishing itself from other receptors, transporters, and kinases. IK-175 is primarily used in research applications focused on studying AHR-related pathways and their implications in various diseases, including cancer and immune responses. -
AHR Antagonist
6,2',4'-Trimethoxyflavone is a potent antagonist of the aryl hydrocarbon receptor (AHR). This compound effectively represses AHR-mediated gene induction, making it a valuable tool for studying AHR-related signaling pathways. Its biological activity supports research in fields such as toxicology, cancer biology, and environmental health. -
AHR Inhibitor
KYN-101 is a selective AHR inhibitor that is potent and orally active. This compound effectively reduces CYP1A1 mRNA expression, contributing to its role in mediating anti-cancer activity. Researchers can utilize KYN-101 to investigate the therapeutic potential in cancer biology and the modulation of AHR-related signaling pathways. -
AhR Agonist
VAF347 is a highly selective aryl hydrocarbon receptor (AhR) agonist that effectively activates AhR signaling pathways. It has been shown to inhibit the differentiation of CD14+CD11b+ monocytes from granulo-monocytic precursors, demonstrating significant anti-inflammatory activity. VAF347 is utilized in research related to immune modulation and the study of inflammatory responses. -
AHR Antagonist
CAY10464 is a selective aryl hydrocarbon receptor (AhR) antagonist with a high affinity, exhibiting a Ki value of 1.4 nM. This compound effectively inhibits AhR signaling, making it valuable for research applications related to toxicology, environmental studies, and the modulation of immune responses. CAY10464 serves as a crucial tool for investigating the role of AhR in various biological processes and disease mechanisms. -
AhR Agonist
AhR Agonist 2 is a highly potent agonist of the aryl hydrocarbon receptor (AhR), exhibiting an EC50 of 0.03 nM. This compound facilitates the nuclear translocation of AhR, leading to the activation of downstream gene transcription and enhancement of skin barrier repair mechanisms. AhR Agonist 2 is valuable for research applications focused on skin conditions, particularly psoriasis. -
AhR activator/Thyroid hormone synthesis and Dopamine beta-hydroxylase inhibitor
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR), functioning as an inhibitor of thyroid hormone synthesis and dopamine beta-hydroxylase activity. This compound promotes the invasion of bladder cancer cells by activating AhR transcription and upregulating the expression of CYP1A1 and CYP1B1, implicated in carcinogenesis. Additionally, 2-Mercaptobenzothiazole exhibits inhibition of thyroid peroxidase activity with an IC50 of 11.5 μM and induces significant histological changes in Xenopus laevis, including delayed metamorphosis. It also increases chromosomal aberrations in Chinese hamster ovary cells and inhibits norepinephrine synthesis in murine models, demonstrating its relevance in carcinogenic studies and neurobiological research. -
AHR Antagonist
CB7993113 is a potent antagonist of the aryl hydrocarbon receptor (AHR), exhibiting an IC50 value of 0.33 μM. This compound effectively binds to the AHR protein and prevents its nuclear translocation, thereby inhibiting the biological effects mediated by this receptor. CB7993113 demonstrates significant inhibitory activity, reducing polycyclic aromatic hydrocarbon (PAH)- and TCDD-induced reporter activity by 75% and 90%, respectively, making it a valuable tool for research into AHR-related signaling pathways and toxicological studies. -
AhR Ligand
10-Cl-BBQ is a high-affinity ligand for the aryl hydrocarbon receptor (AhR), exhibiting significant immunosuppressive activity. This compound facilitates the translocation of AhR from the cytosol to the nucleus and effectively activates AhR-regulated reporter genes at nanomolar concentrations. Its properties make 10-Cl-BBQ a valuable tool for research in immunology and toxicology, particularly in studies focusing on AhR signaling pathways. -
AHR Antagonist
AHR Antagonist 2 is a potent aryl hydrocarbon receptor (AHR) antagonist, displaying IC50 values of 885 pM for human AHR and 2.03 nM for mouse AHR. This compound is valuable for investigations into cancer biology and the modulation of immune responses, making it an important tool for research in immunology and oncology. -
AhR Ligand
Benz[a]anthracene is an aromatic hydrocarbon receptor (AhR) ligand, displaying a pIC50 value of 7.319. As a polycyclic aromatic hydrocarbon (PAH), it is important for studies investigating AhR-mediated biological processes and environmental toxicity. This compound is also relevant in assessing pollution impacts, particularly in samples from areas influenced by industrial activities such as aluminum smelting. -
AhR Agonist
Indolokine A5 is a potent AhR (Aryl hydrocarbon receptor) agonist that plays a significant role in various biological processes. This compound is of particular interest in research applications involving immunology, toxicology, and cancer biology, where AhR activation may influence cellular responses and signaling pathways. Its ability to modulate AhR activity makes Indolokine A5 a valuable tool for studying the effects of environmental contaminants and endogenous ligands on cellular function. -
AhR Activator
3-OH-Kynurenamine (dihydroiodide) is an aryl hydrocarbon receptor (AhR) activator that modulates the immune response. It enhances the expression levels of indoleamine 2,3-dioxygenase 1 (Ido1) and transforming growth factor-beta 1 (Tgfb1). Research indicates that it can alleviate skin inflammation in psoriasis mouse models and mitigate kidney damage in nephrotoxic lupus mouse models, making it a valuable tool in studying immune-related conditions. -
AHR Modulator
DiMNF (3',4'-Dimethoxy-αNF) is a selective modulator of the aryl hydrocarbon receptor (AHR). Acting as a competitive ligand with an IC50 of 21 nM, it exhibits antagonistic properties that can be harnessed in anti-inflammatory research. DiMNF is valuable for investigating the role of AHR in various biological processes and potential therapeutic applications. -
AhR Agonist
N-Methylscatole is an aryl hydrocarbon receptor (AhR) agonist known for its ability to activate this important transcription factor. It exhibits weak agonistic activity and no significant antagonistic properties. This compound can be utilized in research involving AhR-mediated pathways and the study of environmental chemicals affecting biological systems. -
AHR Antagonist
AHR Antagonist 5 is a potent aryl hydrocarbon receptor (AHR) antagonist with an IC50 of less than 0.5 μM. This compound effectively inhibits tumor growth, particularly when used in conjunction with the checkpoint inhibitor anti-PD-1. It serves as a valuable tool for research in cancer biology and the development of combination therapies targeting the immune response. -
AhR antagonist
CHD-5 is a potent antagonist of the aryl hydrocarbon receptor (AhR). This compound effectively inhibits AhR-mediated signaling pathways, which are involved in various biological processes including cellular proliferation and immune responses. CHD-5 is valuable for researchers investigating the role of AhR in cancer biology, immunology, and toxicology. -
AhR Agonist
Corannulene is an agonist of the aryl hydrocarbon receptor (AhR), known for its ability to modulate cellular signaling pathways. This compound exhibits reduced cytotoxicity compared to Benzo[a]pyrene in hepatoma cells, making it a valuable tool in cancer research. Corannulene's unique properties may facilitate the exploration of AhR-related mechanisms in tumor biology and therapeutic interventions. -
hCYP1B1 Inhibitor
hCYP1B1-IN-2 is a highly selective inhibitor of the human cytochrome P450 1B1 enzyme (hCYP1B1). It demonstrates remarkable potency in inhibiting hCYP1B1 activity, with an IC50 value of 0.040 nM, alongside a Ki value of 21.71 pM, indicating effective mixed inhibition. This compound also effectively disrupts aryl hydrocarbon receptor (AhR) transcription activities, making it a valuable tool for research applications focused on cancer and toxicology. -
AHR Inhibitor
AHR-IN-1 is a selective aryl hydrocarbon receptor (AHR) inhibitor, exhibiting an IC50 of less than 0.5 μM. This compound is useful for investigating the role of AHR in various biological processes, including immune response modulation and xenobiotic metabolism. AHR-IN-1 serves as a valuable tool for researchers studying the mechanisms by which AHR influences cellular signaling and gene expression. -
AHR Antagonist
AHR Antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist with a 2-heteroaryl-3-oxo-2,3-dihydropyridazine-4-carboxamide structure, exhibiting an IC50 of 82.2 nM. This compound demonstrates significant anti-cancer properties, making it a valuable tool for research on cancer biology and therapeutic applications targeting AHR pathways. Its ability to modulate AHR signaling may offer insights into mechanisms driving tumor progression and potential treatment strategies. -
AhR Agonist
AhR Agonist 8 is a potent agonist of the Aryl Hydrocarbon Receptor (AhR) with an EC50 value of 0.154 nM. This compound serves as a valuable tool for investigating the biological processes linked to psoriasis and atopic dermatitis. Its high affinity and specificity make AhR Agonist 8 suitable for research applications targeting immune modulation and skin-related disorders. -
hCYP1B1 Inhibitor
CYP1B1-IN-10 is a potent and selective inhibitor of human cytochrome P450 1B1 (hCYP1B1), exhibiting an IC50 value of 0.11 μM. This compound plays a significant role in the investigation of hormone-dependent tumors, including breast and ovarian cancers. Its specificity makes it a valuable tool for studying the therapeutic potential in oncology research. -
AhR Agonist
AhR Agonist 6 is a potent agonist for the aryl hydrocarbon receptor (AhR), exhibiting an EC50 of 0.01 nM. This compound effectively activates AhR signaling pathways, making it valuable for investigating the receptor's role in toxicology, immune response, and cellular differentiation processes. Its high potency allows for precise modulation of AhR-related biological activities in various research applications. -
AhR Activator
3-OH-Kynurenamine is an aryl hydrocarbon receptor (AhR) activator that modulates immune responses. This compound enhances the expression of immune regulatory genes such as Ido1 and Tgfb1, demonstrating therapeutic potential in reducing skin inflammation in psoriasis mouse models, as well as alleviating kidney damage in nephrotoxic lupus mouse models. Its unique biological activity makes it valuable for research involving immune modulation and inflammatory diseases. -
AhR Agonist
AhR agonist 7 is a potent agonist of the aryl hydrocarbon receptor (AhR), exhibiting an EC50 value of 13 nM. This compound effectively activates AhR signaling pathways, making it valuable for research into toxicology, immunology, and cancer biology. AhR agonist 7 can be utilized to study the effects of AhR activation on gene expression and cellular responses. -
AHR Agonis
L-Kynurenine sulfate is an aryl hydrocarbon receptor (AHR) agonist that promotes AHR-mediated signaling pathways. It has been shown to stimulate the polarization of naive T cells towards the anti-inflammatory regulatory T cell (Treg) phenotype, enhancing immune tolerance mechanisms. This compound is valuable for research focused on immunology, inflammation, and therapeutic approaches in autoimmune diseases. -
CYP1A1 Inducer
1,2,3,4,7,8,9-Heptachlorodibenzofuran is a potent inducer of CYP1A1 and CYP1B1 gene expression in human peripheral blood lymphocytes, promoting aryl hydrocarbon receptor repressor (AhRR) transcription. This compound enhances ethoxyresorufin-O-deethylase (EROD) activity, serving as a reliable biomarker for CYP1A1 activation. Additionally, it displays immunosuppressive properties by decreasing the number of splenic plaque-forming cells in mice while increasing aryl hydrocarbon hydroxylase (AHH) activity in liver microsomes. 1,2,3,4,7,8,9-Heptachlorodibenzofuran is valuable for research in immunology, metabolic disorders, and environmental toxicology. -
CYP1A1/1B1 Activator
1,2,3,4,7,8-Hexachlorodibenzofuran is a selective activator of the CYP1A1 and CYP1B1 enzymes. It induces the expression of these cytochrome P450 enzymes and aryl hydrocarbon receptor repressor (AhRR) in human peripheral blood lymphocytes. This compound also stimulates ethoxyresorufin-O-deethylase activity, achieving approximately 20% of the response observed with TCDD at a BMR20TCDD of 0.115-0.143 nM. Its ability to modulate these pathways makes it a valuable tool for studying biological responses to environmental pollutants and the mechanisms of xenobiotic metabolism. -
AHR Activator
AhR modulator-2 is an AHR activator with an EC50 of 0.028 μM in HepG2-Lucia cells. This compound is valuable for investigating the role of the aryl hydrocarbon receptor (AHR) in various diseases, including skin disorders and cancer. Its ability to modulate AHR activity makes it a useful tool in the study of AHR-mediated signaling pathways and associated pathologies. -
Phenylurea Herbicide
Neburon is a phenylurea herbicide that primarily functions by inhibiting photosynthetic electron transport, leading to the disruption of algal growth. This compound activates the aryl hydrocarbon receptor (Ahr) and Notch1 signaling pathways, resulting in the induction of oxidative stress and apoptosis. Prolonged exposure has been associated with significant male reproductive toxicity and cardiotoxicity in zebrafish, making this reagent valuable for studies on environmental impact and toxicological assessments. -
AhR Agonist
Picoberin is a potent aryl hydrocarbon receptor (AhR) agonist that functions at low picomolar concentrations. It is known to inhibit Hedgehog-induced osteoblast differentiation and Wnt3A-induced osteoblast differentiation in C3H10T1/2 cells. Additionally, Picoberin has the ability to upregulate genes responsible for encoding phase I and II metabolic enzymes, making it a valuable reagent for research into cellular differentiation and metabolic processes. -
AHR Antagonist
AHR Antagonist 6 is an aryl hydrocarbon receptor (AHR) antagonist that inhibits AHR signaling pathways. This compound has demonstrated key biological activity in modulating immune responses and is utilized in cancer research to investigate the role of AHR in tumor microenvironments. Researchers can employ AHR Antagonist 6 to explore therapeutic strategies targeting AHR-mediated pathways in various cancer models.
