Catalog No.
Product Name
Application
Product Information
Citations
-
Estrogen Receptor Modulator
Droloxifene is a selective estrogen receptor modulator (SERM) derived from Tamoxifen. It exhibits antiestrogenic and anti-implantation properties, making it relevant for research in reproductive health. In cellular studies, Droloxifene has been shown to induce p53 expression and promote apoptosis in MCF-7 breast cancer cells. Additionally, it demonstrates protective effects against bone loss in ovariectomized rat models, highlighting its potential applications in osteoporosis research. -
ERα Inhibitor
Isocurcumenol is an estrogen receptor alpha (ERα) inhibitor derived from the rhizomes of Curcuma zedoaria. It demonstrates significant anti-tumor activity, exhibiting IC50 values of 99.1 μg/mL in Dalton's lymphoma ascites (DLA) cells and 178.2 μg/mL in KB cells. This compound has potential applications in cancer research, particularly in exploring targeted therapies for hormone-dependent tumors. -
GR/IL-6 Inhibitor
Glucocorticoid receptor/IL-6-IN-1 is a selective dual inhibitor that targets both the glucocorticoid receptor (GR) and the IL-6 signaling pathway, demonstrating IC50 values of 120 nM and 59 nM, respectively. This compound effectively inhibits IL-6-induced phosphorylation of JAK/STAT3, thereby blocking the transcription of inflammatory cytokines. Glucocorticoid receptor/IL-6-IN-1 is a valuable tool for investigating inflammatory diseases, including rheumatoid arthritis and asthma. -
Renin Inhibitor
Aliskiren fumarate is a potent and selective renin inhibitor with an IC50 of 1.5 nM. It is primarily utilized in research related to hypertension and cardiovascular diseases, as well as cancer cachexia. Its mechanism of action involves the inhibition of renin, a key enzyme in the regulation of blood pressure, making it an important tool for studying these conditions. -
Renin Inhibitor
Aliskiren hydrochloride is a potent and selective renin inhibitor, exhibiting an IC50 of 1.5 nM. This compound is widely used in the study of hypertension and cardiovascular diseases, as well as in research related to cancer cachexia. Its ability to modulate renin activity makes it a valuable tool for exploring the pathophysiological mechanisms underlying these conditions. -
Stable Isotope
Mifepristone-d6 is a deuterated form of Mifepristone, a potent antagonist of the progesterone receptor (PR) and the glucocorticoid receptor (GR), exhibiting IC50 values of 0.2 nM and 2.6 nM, respectively, in in vitro assays. This stable isotope-labeled compound serves as a valuable tool for metabolic studies, pharmacokinetic investigations, and research on receptor interactions. Its unique isotopic signature allows for precise tracking and analysis in biological systems, facilitating advanced research in endocrinology and reproductive health. -
hGPR132a Antagonist
GSK1820795A is a selective antagonist of the human GPR132a receptor, effectively inhibiting its activation by N-acylamides in yeast cell models. This compound also functions as an antagonist of angiotensin II and has partial agonist activity at PPARγ. It serves as a valuable tool for research into metabolic disorders and receptor signaling pathways. -
FFA1/GPR40 Agonist
HWL-088 is a potent agonist of free fatty acid receptor 1 (FFA1/GPR40) with an EC50 of 18.9 nM, exhibiting moderate activity on PPARδ with an EC50 of 570.9 nM. This compound enhances glucose and lipid metabolism, demonstrating significant anti-diabetic effects. HWL-088 is valuable for research investigating metabolic disorders and insulin sensitivity. -
ERRγ Inverse Agonist
(E/Z)-GSK5182 is a racemic mixture of the (E)- and (Z)-isomers that acts as a selective inverse agonist of estrogen-related receptor γ (ERRγ), exhibiting an IC50 of 79 nM. This compound is notable for its ability to induce the generation of reactive oxygen species (ROS), particularly in hepatocellular carcinoma models. Due to its specificity and biological activity, (E/Z)-GSK5182 is a valuable tool for investigating ERRγ-related signaling pathways and potential therapeutic applications in cancer research. -
Glucocorticoid Receptor Agonist
Beclometasone dipropionate monohydrate is a potent glucocorticoid receptor agonist with significant anti-inflammatory properties. It functions through the activation of the glucocorticoid receptor, effectively suppressing inflammation and cellular hyperproliferation. This compound is primarily utilized in research related to asthma treatment and the modulation of inflammatory responses. -
GPR35 Activator
DHICA is a GPR35 agonist that acts as both an eumelanin building block and a melanin synthesis intermediate. It activates GPR35, leading to dynamic mass redistribution and β-arrestin translocation. Additionally, DHICA promotes single-strand breaks in plasmid DNA and enhances the activity and expression levels of superoxide dismutase (SOD) and catalase. This compound is relevant for research applications in skin cancer and colon cancer studies. -
HGPRT Inhibitor
8-Azahypoxanthine is a purine analog that functions as an inhibitor of hypoxanthine-guanine phosphoribosyltransferase (HGPRT). This compound demonstrates antitumor activity, making it a valuable tool in cancer research, particularly for studying adenocarcinoma and other tumor types. Its ability to inhibit HGPRT may provide insights into the mechanisms of tumor growth and potential therapeutic strategies. -
GPR17 Antagonist
RWT9996 is a selective antagonist of GPR17, functioning by inhibiting G protein activation and β-arrestin-2 recruitment prompted by MDL-29951. This compound effectively reduces ERK/CREB phosphorylation and the accumulation of inositol phosphates in response to MDL-29951 stimulation. RWT9996 is valuable for research into neurological disorders, providing insights into the role of GPR17 in various pathophysiological processes. -
GPR55 Agonist
20:4 Lyso PI is a selective agonist of the G protein-coupled receptor GPR55, exhibiting a potency with an EC50 value of 10 nM in inducing cell rounding in GPR55-expressing HEK293 cells. This compound activates RhoA, leading to ROCK-dependent cytoskeletal rearrangement, and stimulates the ERK signaling pathway while increasing intracellular free calcium levels. 20:4 Lyso PI is valuable for research into immune diseases and related cellular signaling mechanisms. -
GnRH Receptor Antagonist
SKI2496 is a potent GnRH receptor antagonist that exhibits an IC50 of 0.25 nM for human GnRHR, demonstrating high specificity across species with values of 13.2 nM for monkey and 279.2 nM for rat receptors. This compound effectively inhibits Ca2+ influx with an IC50 of 0.76 nM and blocks ERK1/2 phosphorylation with an IC50 of 2.6 nM. SKI2496 is utilized in research focused on sex hormone-dependent disorders, particularly for its ability to reduce serum LH concentrations. -
GPR119 Agonist
2-Oleoylglycerol is a GPR119 agonist that activates hGPR119 in transiently transfected COS-7 cells with an EC50 value of 2.5 μM. This lipid enhances the inflammatory response in macrophages and promotes fibrosis through the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. Additionally, 2-Oleoylglycerol stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. Its effects make it a valuable tool for research into non-alcoholic steatohepatitis (NASH) and related metabolic disorders. -
Glucocorticoid Receptor Ligand
PF-04308515 is a selective glucocorticoid receptor ligand that exhibits significant anti-inflammatory properties. It effectively inhibits the production of interleukin-6 (IL-6) and interferon gamma (IFNγ), making it a valuable tool for studying inflammation and immune responses. Additionally, PF-04308515 induces a weak interaction with PGC1α, providing insights into its potential metabolic effects. This compound is useful for research applications focused on inflammation, autoimmune diseases, and glucocorticoid signaling pathways. -
GR/IL-6 Inhibitor
Glucocorticoid receptor/IL-6-IN-2 is a selective dual inhibitor targeting the glucocorticoid receptor (GR) and the IL-6 signaling pathway, with IC50 values of 40 nM and 19 nM, respectively. This compound has demonstrated significant potential in inhibiting inflammatory responses, making it a valuable tool for research into inflammatory diseases such as rheumatoid arthritis and asthma. Its unique mechanism of action allows for exploration of therapeutic strategies aimed at modulating immune responses and mitigating chronic inflammation. -
Progesterone Receptor Antagonist
Trimegestone acts as a progesterone receptor antagonist, exhibiting a high binding affinity with an IC50 value of 3.3 nM for the rat progesterone receptor. This 19-norpregnane progestin enhances alkaline phosphatase activity, with an EC50 of 0.1 nM, while displaying minimal effects on luciferase activity. Additionally, Trimegestone possesses weak antiandrogenic properties due to its low affinity for the androgen receptor. This compound is valuable in research focusing on contraception and menopausal syndrome investigations. -
GPR34 Receptor Antagonist
GPR34 Receptor Antagonist 2 is an antagonist that specifically targets the GPR34 receptor. This compound exhibits significant activity in modulating immune responses, making it a valuable tool for investigating inflammatory diseases and other immune-related disorders. Its potential applications in research include studying the pathophysiology of immune diseases and developing novel therapeutic strategies. -
GPR34 Receptor Antagonist
GPR34 receptor antagonist 3 is a selective antagonist of the GPR34 receptor, with an IC50 value of 0.680 μM. This compound effectively inhibits ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent manner, demonstrating minimal cytotoxicity. GPR34 receptor antagonist 3 is valuable for research into the modulation of sensory signaling pathways and has shown antisensory activity in mouse models of neuropathic pain. -
Androgen Receptor Antagonist
Deutenzalutamide-d3 is a deuterium-labeled analog of Enzalutamide, an androgen receptor (AR) antagonist. It exhibits potent activity with an IC50 of 36 nM in LNCaP prostate cancer cells. This reagent is valuable for studying androgen receptor signaling pathways and resistance mechanisms in prostate cancer research. -
GPR35 Agonist
Bufrolin is a potent agonist of GPR35, known for its ability to promote the interaction between β-arrestin-2 and both human GPR35a and rat GPR35. This compound exhibits significant antiallergic properties by stabilizing mast cells and inhibiting inflammatory responses associated with internalization peptides. Bufrolin is valuable for research into anti-inflammatory mechanisms and therapeutic applications targeting GPR35-related pathways. -
Glucocorticoid Receptor Activator
Flunisolide hemihydrate is an orally active glucocorticoid receptor activator with potent anti-inflammatory properties. It induces eosinophil apoptosis, making it a valuable tool for researchers investigating asthma, rhinitis, and various inflammatory conditions. Its mechanism of action supports studies focused on the modulation of inflammatory pathways and the therapeutic applications of corticosteroids in respiratory diseases. -
ERα Degrader
ERα degrader 14 is a selective degrader of estrogen receptor alpha (ERα), primarily functioning through targeted proteasomal degradation. This compound demonstrates potent anti-proliferative effects in ERα-positive breast cancer cell lines, including MCF-7 and T47D, by inducing cell cycle arrest, inhibiting cell migration, and promoting apoptosis. Additionally, ERα degrader 14 effectively suppresses tumor growth in in vivo mouse models, making it a valuable tool for research in breast cancer biology and therapeutic development. -
Estrogen Receptor Modulator
rel-Levormeloxifene is a selective estrogen receptor modulator (SERM) that primarily targets estrogen receptors. This compound effectively inhibits the proliferation of leukemia cells, demonstrating an IC50 of approximately 7 μM. Additionally, rel-Levormeloxifene induces cell cycle arrest at the G0/G1 phase and promotes apoptosis. It also facilitates myelogenesis differentiation while enhancing reactive oxygen species (ROS) production in K562 cells, making it a valuable reagent for research in leukemia and related hematological disorders. -
Androgen Receptor Degrader
ZC9 is a novel androgen receptor (AR) degrader that directly binds to AR, inhibiting its Dihydrotestosterone-induced nuclear translocation. By promoting AR degradation through the ubiquitin-proteasome system, ZC9 effectively suppresses AR transcriptional activity, leading to a significant decrease in the mRNA levels of downstream genes such as PSA, TMPRSS2, and PMEPA1. Additionally, ZC9 induces apoptosis and demonstrates notable anticancer effects in prostate cancer models, making it a valuable tool for research in androgen signaling and cancer therapeutics. -
Estrogen Receptor
BMI-135 is a selective estrogen receptor agonist that mimics estrogen activity. This compound has been shown to induce a rapid endoplasmic reticulum stress response (unfolded protein response, UPR) and promote apoptosis in breast cancer cells. BMI-135 serves as a valuable tool for studying the mechanisms of estrogen signaling and the therapeutic potential of targeting estrogen receptors in breast cancer research. -
Estrogen Receptor Epitope
ERα17p is an epitope derived from the CaM binding site on estrogen receptor alpha (ERα), facilitating its interaction with calmodulin (CaM) in a calcium-dependent manner. This peptide has been shown to regulate the migration of various breast cancer cell lines, including MCF-7, SK-BR-3, T47D, and MDA-MB-231, by activating Rho/ROCK and PI3K/Akt signaling pathways. Additionally, ERα17p exhibits inhibitory effects on breast cancer cell proliferation, induces apoptosis, and suppresses tumor growth in murine models, making it a valuable tool for cancer research. -
Estrogen Receptor Agonist, Voltage-Gated Sodium Channel Blocker, PI3K-AKT/JNK Signaling Modulator,
Propylparaben sodium acts as a weak estrogen receptor agonist and serves as a voltage-gated sodium channel blocker, while also modulating the PI3K-AKT and JNK signaling pathways. It is known to induce oxidative stress, affecting the estrous cycle and hormone levels, as well as ovarian reserve function. Propylparaben sodium can inhibit the growth of antral follicles and influence the accumulation of steroid hormones in follicle culture media. This compound is suitable for research related to ovarian aging and myocardial ischemia-reperfusion injury. -
Androgen Receptor Antagonist
AR Antagonist 15 is an orally bioavailable antagonist of the androgen receptor (AR), exhibiting an IC50 of 97 nM for ART787A. This compound inhibits AR nuclear translocation, prevents AR homodimerization, and suppresses transcription of AR-regulated genes through competitive binding at the ligand binding pocket. Additionally, AR Antagonist 15 significantly reduces prostate-specific antigen (PSA) levels and induces apoptosis by decreasing the expression of proteins involved in apoptotic pathways. This reagent is relevant for studies investigating the mechanisms of prostate cancer. -
ERα Degarder
X15695 is a selective estrogen receptor alpha (ERα) degrader that functions as an aryl hydrocarbon receptor (AHR) ligand. By facilitating the formation of a complex between AHR and ERα, X15695 promotes the proteasomal degradation of ERα, leading to the inhibition of breast cancer cell proliferation. Additionally, it induces cell cycle arrest and apoptosis. This compound is valuable for research in breast cancer biology and therapeutics. -
GPR91 Ligand
Succinate calcium primarily targets the G protein-coupled receptor GPR91 and serves as a significant intermediate in the citric acid cycle. This compound is known to enhance the amplitude of calcium transients in cardiac muscle cells while also accelerating their decay rate. Additionally, succinate calcium has been implicated in inducing myocardial apoptosis, making it valuable for research into cardiac physiology and pathology. -
Progesterone Receptor Modulator
Telapristone acetate is a potent progesterone receptor modulator that effectively inhibits the proliferation of ovarian cancer cells by inducing cell cycle arrest and apoptosis. This compound has demonstrated efficacy in reducing the incidence and progression of both spontaneous and chemically induced mammary tumors in animal models. Telapristone acetate is valuable for research focused on breast and ovarian cancer, providing insights into its therapeutic potential and mechanisms of action. -
ERα Antagonist
ER covalent antagonist-1 is a selective antagonist of estrogen receptor α (ERα). It effectively inhibits the proliferation of ERα-positive MCF-7 cells, with an IC50 value of 0.98 μM, and promotes cell cycle arrest in the G0/G1 phase while inducing apoptosis. In vivo studies demonstrate its significant antitumor efficacy in mouse models, highlighting its potential for research in cancer therapeutics targeting estrogen signaling pathways. -
Androgen Receptor Inhibitor
Androgen receptor-IN-7 is a potent inhibitor of the androgen receptor (AR), demonstrating significant anticancer activity against PC-3 (IC50 = 370.37 nM) and LNCaP cell lines through both AR-dependent and AR-independent mechanisms. This compound induces reactive oxygen species (ROS) production in PC-3 cells, highlighting its potential role in oncological studies. Androgen receptor-IN-7 is useful for research focused on prostate cancer and related therapeutic strategies. -
GPR84 Antagonist
TUG-2181 is a GPR84 antagonist, exhibiting an IC50 value of 34 nM. This compound effectively inhibits reactive oxygen species (ROS) production and interleukin-8 (IL-8) release in human neutrophils stimulated by GPR84 agonists. TUG-2181 is particularly valuable for research exploring the mechanisms of inflammation and fibrosis. -
RORγ/DHODH Inhibitor
RORγ/DHODH-IN-1 is a dual inhibitor targeting RORγ and dihydroorotate dehydrogenase (DHODH) with IC50 values of 9.7 nM and 100 nM, respectively. This compound effectively inhibits the replication of SARS-CoV-2, human cytomegalovirus (HCMV), and adenovirus type 5 (HAdV5), making it a valuable tool in viral research. Its dual mechanism of action allows for potential applications in understanding viral-pathogen interactions and developing therapeutic strategies against viral infections. -
RORγt Inverse Agonist
BMS-986251 is a selective RORγt inverse agonist with an EC50 of 12 nM in RORγt GAL4 assays. It effectively inhibits IL-17 production with an EC50 of 24 nM in human whole blood assays. BMS-986251 exhibits significant efficacy in preclinical models of psoriasis, including mouse acanthosis and Imiquimod-induced models, making it a valuable tool for research in autoimmune and inflammatory diseases. -
Androgen Receptor Inhibitor
Ac-PPPHPHARIK-NH2 is an androgen receptor inhibitor that disrupts the interaction between the androgen receptor and Src. By preventing this binding, it effectively inhibits androgen or estrogen-induced receptor activation in cancer cells, thereby modulating related signaling pathways. This compound has been shown to impede cell cycle progression and suppress tumor growth, making it a valuable tool for research in cancer biology and hormone receptor signaling. -
Stable Isotope
Dexamethasone-4,6α,21,21-d4 is a deuterated derivative of Dexamethasone, functioning as a glucocorticoid receptor agonist. It exhibits potent anti-inflammatory properties, including the modulation of neutrophil and monocyte surface markers such as CD11b and CD18, which are crucial for immune cell activation and migration. This reagent is particularly relevant for research on inflammatory responses, including studies related to COVID-19, as well as investigations into exosome-mediated microRNA regulation in macrophage activation. -
Stable Isotope
Dexamethasone-d5 is a deuterium-labeled analog of the glucocorticoid receptor agonist Dexamethasone. It is known to reduce the expression of CD11b, CD18, and CD62L on neutrophils, as well as CD11b and CD18 on monocytes, thereby modulating immune responses. This stable isotope is particularly valuable in research applications studying the mechanics of inflammation, including the regulation of exosomal microRNA-155 production in lipopolysaccharide-stimulated macrophages, and its efficacy in managing conditions such as COVID-19. -
Stable Isotope
Dexamethasone-d4 is a deuterium-labeled derivative of Dexamethasone, which acts as a potent glucocorticoid receptor agonist. This compound has notable biological activities, including the modulation of immune cell marker expression by decreasing levels of CD11b, CD18, and CD62L on neutrophils, as well as CD11b and CD18 on monocytes. Dexamethasone-d4 is particularly valuable for research applications related to anti-inflammatory responses and the investigation of COVID-19 pathophysiology, as it inhibits exosome production containing inflammatory microRNA-155 during macrophage activation. -
GnRH Antagonist
Teverelix is a GnRH antagonist that binds competitively and reversibly to GnRH receptors, inhibiting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This compound plays a critical role in the study of disorders related to reproductive hormone regulation, including prostatic hyperplasia, endometriosis, and prostate cancer. Its selective mechanism makes it a valuable tool for research in endocrinology and oncology. -
GPR75 Inhibitor
(Rac)-AAA is a potent inhibitor of GPR75, targeting the receptor to modulate key signaling pathways. This compound effectively blocks the downregulation of GPR75 expression induced by 20-HETE, leading to the inhibition of downstream pathways such as EGFR, AKT, NF-κB, and FAK. (Rac)-AAA also reverses 20-HETE-mediated epithelial-mesenchymal transition, characterized by the downregulation of vimentin and upregulation of E-Cadherin, while reducing MMP-2 activity and cancer cell migration. Additionally, it mitigates the upregulation of HIC-5 and affects the localization of PKC-α and phosphorylated AKT, making (Rac)-AAA a significant tool in the study of castration-resistant prostate cancer. -
Androgen Receptor antagonist
(R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells. -
Androgen antagonist
17 alpha-propionate is a new topical and peripherally selective androgen antagonist. -
Aromatase inhibitor
Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids. -
Androgen Receptor agonist
Andarine (GTX-007) is an investigational selective androgen receptor modulator (SARM). -
RAAS inhibitor
Benazepril hydrochloride is a non-peptide angiotensin-converting enzyme (ACE) inhibitor. Reduces blood pressure and myocardial hypertrophy in spontaneous hypertensive rats.
