Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
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. -
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. -
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. -
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. -
Drug-Linker Conjugate for ADC
Glucocorticoid receptor modulator 4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications. This compound demonstrates glucocorticoid receptor (GRE) reporter activation in mTNF-expressing K562 cells with an EC50 of 40 μM. Additionally, it exhibits binding affinity with anti-tumor necrosis factor (TNF) antibodies and exhibits anti-inflammatory effects in mouse models of arthritis, making it a valuable tool for research in inflammation and autoimmune diseases. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-1 phosphate Gly-Glu-Mal is a glucocorticoid receptor agonist designed for targeted drug delivery applications. This compound functions as a linker in antibody-drug conjugates (ADCs) and facilitates the synthesis of anti-CD40 antibody conjugates for therapeutic research. Its modulation of glucocorticoid receptor activity makes it valuable for studies investigating immune response and inflammation targets. -
Estrogen Receptor Targeting Agent
Fluoroestradiol is an estrogen receptor-targeting agent utilized as a PET imaging tracer for the assessment of estrogen receptor expression. When radiolabeled with 18F, Fluoroestradiol demonstrates high uptake selectivity and an optimal target-to-background ratio, making it particularly effective in distinguishing estrogen receptor activity in various tissues. This reagent has applications in quantifying estrogen receptor expression in breast cancer and monitoring heterogeneity in ovarian cancer, as well as revealing estrogen receptor presence in normal brain tissues and meningiomas. -
ROR2 ADC
Ozuriftamab vedotin is an antibody-drug conjugate (ADC) targeting the receptor tyrosine kinase orphan receptor 2 (ROR2). This compound combines a humanized monoclonal antibody, Ozuriftamab, with the cytotoxic agent VcMMAE, enabling selective delivery to ROR2-expressing tumor cells. Ozuriftamab vedotin exhibits potent antitumor activity and is utilized in research focused on cancer therapeutics and targeted therapies. -
ROR1 ADC Intermediate
BL20-MMAE is an antibody-drug conjugate designed to target the receptor tyrosine kinase ROR1. This compound is synthesized by linking an anti-ROR1 antibody with the cytotoxic agent MMAE through a BL20 linker, facilitating targeted delivery of the drug. BL20-MMAE is primarily utilized in research applications focused on cancer therapeutics, particularly in studies involving ROR1-positive malignancies. -
FKBP51 Degrader, VHL Binder
SelDeg51 is a selective PROTAC degrader targeting FKBP51 with a Kd value of 18 nM and a maximum degradation efficacy (Dmax) of 90%. It facilitates the proteasomal degradation of FKBP51 through the formation of a ternary complex with FKBP51 and VHL, effectively reactivating glucocorticoid receptor signaling. SelDeg51 is particularly relevant for research in stress-related mental disorders, chronic pain, and obesity. -
Glucocorticoid Receptor Agonist
Glucocorticoid Receptor Agonist-1 is a highly potent glucocorticoid receptor agonist with an IC50 of 2.8 nM. This compound modulates the glucocorticoid receptor, influencing a variety of physiological processes including inflammation and immune responses. It is suited for research applications aimed at exploring mechanisms of glucocorticoid signaling and its implications in diseases such as asthma, arthritis, and other inflammatory conditions. -
GR Agonist
Glucocorticoid receptor agonist-2 is a potent agonist of the glucocorticoid receptor (GR) with an IC50 value of 6.6 nM. This compound is instrumental in synthesizing anti-inflammatory antibody-drug conjugates (ADCs), making it valuable for research in inflammation and immune response modulation. Its effectiveness as an active reference in studies related to GR-targeted therapies supports its applicability in therapeutic development. -
Glucocorticoid Receptor Agonist
Glucocorticoid Receptor Agonist-5 is a potent agonist of the glucocorticoid receptor. This compound exhibits significant anti-inflammatory and immunosuppressive properties, making it valuable in research focused on inflammatory diseases and immune response modulation. Additionally, it serves as an antibody-drug conjugate (ADC) cytotoxin, facilitating targeted therapeutic approaches in cancer research. -
Glucocorticoid Receptor Agonist
Glucocorticoid receptor agonist-4 is a selective agonist for the glucocorticoid receptor, offering insights into the modulation of inflammatory processes. This compound can be conjugated to TNF-α antibodies, facilitating research into autoimmune and inflammatory diseases. Its applications extend to the study of glucocorticoid signaling pathways and therapeutics in related conditions. -
Glucocorticoid Receptor Agonist
Glucocorticoid Receptor Agonist-3 is an effective agonist that targets the glucocorticoid receptor. It exhibits significant anti-inflammatory and immunomodulatory activities, making it valuable for research in the fields of inflammation, autoimmune diseases, and hormone signaling. This compound is essential for studying the therapeutic potential of glucocorticoids in various biological contexts. -
GR Agonist
Glucocorticoid receptor agonist-6 is a specific agonist for the glucocorticoid receptor (GR). It exhibits significant cytotoxic activity, making it an excellent candidate for use as a payload in the synthesis of antibody-drug conjugates (ADCs). This compound supports research in targeted therapy approaches for diseases where GR modulation is beneficial.
