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Catalog No.
Product Name
Application
Product Information
Citations
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Renin Inhibitor
PD125754 is a potent oligopeptide inhibitor of renin, exhibiting an IC50 of 22 nM. This compound effectively reduces renin activity, making it valuable for studies related to hypertension and cardiovascular diseases. Its ability to modulate the renin-angiotensin system can aid in the exploration of mechanisms underlying renal and cardiovascular function. -
Renin Inhibitor
SC-46944 is an orally active renin inhibitor that effectively targets the renin-angiotensin system. It demonstrates significant potential in the study of hypertension by reducing renin activity and subsequently lowering blood pressure. This compound serves as a valuable tool in cardiovascular research and the development of antihypertensive therapies. -
Human Renin Inhibitor
ES 6864 is a potent, orally active competitive inhibitor of human renin, demonstrating an IC50 of 6.9 nM and a Ki of 7.3 nM. It possesses high specificity for both species and enzyme, making it a valuable tool in cardiovascular research. Additionally, ES 6864 exhibits metabolic stability in rat tissue homogenates and effectively lowers blood pressure in rat models and sodium-depleted awake marmosets, supporting its potential applications in hypertension studies. -
Renin Inhibitor
ACT 178882 is a potent renin inhibitor with an IC50 of 1.4 nM. It effectively modulates the renin-angiotensin-aldosterone system, leading to potential applications in the treatment of hypertension and related cardiovascular disorders. This compound serves as a valuable tool for research into the role of renin in blood pressure regulation and the development of novel antihypertensive therapies. -
TH17 Cell Differentiation Inhibitor
3-Oxo-5β-cholanoic acid, also known as Dehydrolithocholic acid, functions as a potent inhibitor of TH17 cell differentiation. This compound achieves its biological activity by directly binding to the transcription factor RORγt, with a dissociation constant (Kd) of 1.13 μM. It is useful in research applications aimed at understanding inflammatory responses and immune modulation. -
RORγt Inhibitor
GSK805 is an orally active RORγt inhibitor that effectively modulates immune responses. Its mechanism involves inhibiting RORγ and the differentiation of Th17 cells, demonstrating pIC50 values of 8.4 and >8.2, respectively. GSK805 further suppresses Th17 cell functionality, making it a valuable tool for investigating immune-related disorders and therapeutic approaches targeting RORγt in inflammatory conditions. -
ROR1 Inhibitor
LDR102 is a potent inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) with a Ki value of 0.10 μM. This compound effectively inhibits the proliferation of various cancer cell lines, including H1975, A549, and MDA-MB-231, exhibiting IC50 values of 0.36 μM, 1.37 μM, and 0.47 μM, respectively. Additionally, LDR102 demonstrates antitumor efficacy in murine models and displays favorable pharmacokinetic properties in rat studies, making it a valuable tool for cancer research and therapeutic development. -
ROR-γ Inhibitor
JTE-151 is a potent ROR-γ inhibitor that effectively modulates immune responses by inhibiting ROR-γ activity associated with the activation of Th17 cells. This mechanism allows JTE-151 to serve as a valuable tool in the study of autoimmune diseases and related immunological disorders. By suppressing the overactive immune response, it holds promise for advancing research in therapeutic strategies targeting autoimmune conditions. -
RORγt Inhibitor
Vimirogant hydrochloride is a potent and selective RORγt inhibitor, displaying a Ki of 3.5 nM and an IC50 of 17 nM. This compound demonstrates over 1000-fold selectivity for RORγt compared to RORα and RORβ isotypes. Vimirogant hydrochloride effectively inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes with an IC50 of 57 nM, while sparing Th1, Th2, and Treg cell differentiation. This specificity positions Vimirogant hydrochloride as a valuable reagent for research into autoimmune disorders. -
ROR Inhibitor
RORγt Inhibitor 1 is a potent allosteric inhibitor of RORγt, exhibiting an IC50 value of 1 nM. This compound effectively modulates RORγt activity, playing a crucial role in the regulation of immune responses. It is primarily utilized in research related to autoimmune diseases and metabolic disorders, providing valuable insights into the therapeutic potential of RORγt inhibition. -
RORγt Inhibitor
RORγt Inhibitor 4 is a potent inhibitor of the RORγt transcription factor, specifically designed for oral administration and capable of penetrating the central nervous system. This compound demonstrates significant efficacy in modulating immune responses, making it valuable for research into autoimmune conditions, particularly in the context of experimental autoimmune encephalomyelitis. Its ability to selectively inhibit RORγt activity positions it as a promising tool for investigating therapeutic strategies in autoimmune diseases. -
RORγt Inhibitor
RORγt Inhibitor 2 is a selective inhibitor of the RORγt transcription factor, exhibiting an IC50 value of 9.2 nM. This compound demonstrates significant anti-inflammatory and immunomodulatory activity, making it a valuable tool for research into cancer, autoimmune disorders, and inflammatory conditions driven by RORγt signaling. Its specificity and potency enable detailed studies of RORγt's biological roles and therapeutic potential. -
RORγ Inhibitor
RORγ-IN-2 is a selective inhibitor of RAR-related orphan receptor gamma (RORγ) with a Ki of 16.6 nM for human RORγ. This compound is primarily utilized in research focused on IL-17-dependent autoimmune diseases, providing insights into the modulation of immune responses and inflammation. RORγ-IN-2 serves as a valuable tool for investigating the therapeutic potential of targeting RORγ in various pathological conditions. -
AR Inhibitor
AR ligand-48 is an inhibitor of the Androgen Receptor (AR), functioning as a ligand for PROTAC applications. By targeting the AR, this compound facilitates the development of PROTAC AR Degrader-12, enabling researchers to investigate AR degradation pathways. Its utility in studying androgen signaling makes it valuable for research in hormone-related diseases and therapeutic development. -
STS Inhibitor/ERα Modulator
SR-16157 is a dual-action steroid sulfatase (STS) inhibitor and selective estrogen receptor alpha (ERα) modulator, with an IC50 of 0.1 µM. This compound displays potent STS inhibitory and anti-estrogenic effects in breast cancer cells, making it a valuable tool for understanding the role of estrogen signaling in cancer progression. SR-16157 is applicable in breast cancer research, particularly in studies exploring therapeutic strategies targeting estrogen metabolism and receptor modulation. -
Estrogen Receptor/ERR Inhibitor
BHPI is a selective inhibitor of the estrogen receptor ERα, regulating downstream signaling pathways by activating phospholipase C gamma (PLCγ) and inducing the unfolded protein response (UPR). This compound exhibits significant antitumor activity, making it relevant for research in breast, endometrial, and ovarian cancers. Its ability to modulate estrogen-related signaling pathways positions BHPI as a valuable tool in the study of hormone-driven malignancies and therapeutic interventions. -
Androgen Receptor Inhibitor
Ailanthone (Δ13-Dehydrochaparrinone) is a potent inhibitor of the androgen receptor, exhibiting an IC50 of 69 nM for full-length AR and 309 nM for constitutively active truncated AR splice variants (AR1-651). Its ability to selectively target these receptors makes it a valuable tool for research into androgen signaling pathways. Ailanthone is applicable in studies related to prostate cancer and other conditions influenced by androgen receptor activity. -
Androgen Receptor Inhibitor
Masofaniten is a potent androgen receptor inhibitor, functioning through the selective modulation of androgen receptor activity. It exhibits significant antitumor efficacy against prostate cancer, making it a valuable tool for studying androgen signaling pathways and exploring therapeutic options for prostate cancer treatment. Researchers can utilize Masofaniten to investigate the biological mechanisms of androgen receptor antagonism and its potential in cancer therapy. -
NONO Inhibitor
(R)-SKBG-1 is a covalent inhibitor that targets the RNA binding protein NONO. This compound effectively reduces the expression of the androgen receptor (AR) and its splice variants, demonstrating an IC50 of 3.1 µM for AR-FL mRNA and 5.5 µM for AR-V7 mRNA. By stabilizing the interaction between NONO and mRNA, (R)-SKBG-1 disrupts the gene regulatory networks in cancer cells, thereby inhibiting cell proliferation. This reagent is valuable in research focusing on cancers associated with NONO dysfunction, including prostate cancer. -
AR-DBD Inhibitor
VPC-14449 is a selective inhibitor targeting the DNA-binding domain of the androgen receptor (AR-DBD), demonstrating an IC50 value of 0.34 μM for full-length human AR. This compound effectively diminishes the binding capacity of both full-length AR and its variants to chromatin, thereby influencing androgen receptor-mediated transcription. VPC-14449 is valuable for research focused on prostate cancer and the role of AR in tumor progression. -
Ar-V7 Inhibitor
Ar-V7-IN-1 is a potent inhibitor of the androgen receptor variant 7 (Ar-V7), effectively inhibiting its transcriptional activity. This compound demonstrates an eGFP IC50 value of 1232 nM and a PSA IC50 of 1391 μM. Ar-V7-IN-1 is primarily utilized in research related to prostate cancer, making it a valuable tool for investigating the mechanisms of AR-mediated signaling and the associated implications in cancer biology. -
AR-DBD Inhibitor
VPC-14228 is a selective inhibitor of the androgen receptor DNA binding domain (AR-DBD). It interrupts the interaction between the androgen receptor and DNA, thereby preventing AR-mediated transcriptional activation. VPC-14228 effectively inhibits the activity of both full-length androgen receptors and the splice variant AR-V7 by disrupting AR binding to chromatin, demonstrating high selectivity for other nuclear receptors such as estrogen and progesterone receptors. This compound is applicable for research into prostate cancer. -
Androgen Receptor Inhibitor/GPR142 Antagonist
CLP-3094 is a selective androgen receptor (AR) inhibitor that targets the binding function 3 (BF3) region, effectively reducing AR transcriptional activity with an IC50 of 4 μM. In addition, CLP-3094 serves as a potent antagonist of GPR142, making it a valuable compound for research into androgen receptor modulation and its implications in various biological processes. Its dual function positions CLP-3094 as a useful tool in studies related to androgen signaling and GPR142-related pathways. -
Androgen Receptor Inhibitor
ET516 is a potent inhibitor of the Androgen Receptor (AR), effectively disrupting AR signaling pathways. This compound demonstrates significant anti-proliferative effects and inhibits tumor growth in prostate cancer cells with AR-resistant mutants. ET516 is valuable for research applications focused on understanding AR-related mechanisms in prostate cancer and developing targeted therapies. -
Androgen Receptor Inhibitor
Androgen receptor-IN-6 is a potent inhibitor of the androgen receptor, specifically targeting the disordered N-terminal domain (NTD) with an in vitro IC50 of 0.12 μM. This compound demonstrates favorable membrane permeability in Caco2 cells and exhibits oral bioavailability in male CD-1 mice, with an F/% of 16%. It serves as a valuable tool for research into androgen receptor signaling pathways and the development of therapeutic strategies for androgen-dependent conditions. -
AR NTD Inhibitor
Ralaniten triacetate is an orally active inhibitor that targets the N-terminal domain (NTD) of the androgen receptor (AR). This first-in-class compound demonstrates efficacy against full-length androgen receptors as well as resistance-related variants, including AR-v7. It is primarily utilized in research focusing on androgen receptor signaling pathways and their role in hormone-driven cancers. -
Androgen Receptor Inhibitor
A4B17 is an androgen receptor N-terminal inhibitor that selectively targets the androgen receptor, interfering with its transcriptional activity. It is primarily used in research related to androgen-responsive prostate cancer, allowing for investigations into therapeutic strategies and mechanisms of resistance. A4B17 provides a valuable tool for studying androgen receptor signaling pathways and their implications in tumor progression. -
AR Inhibitor
VPC-13566 is a selective inhibitor of the androgen receptor (AR), exerting its effects via inhibition of AR transcriptional activity. This compound effectively suppresses the proliferation of AR-dependent prostate cancer cell lines in vitro. VPC-13566 is a valuable tool for investigating the AR signaling pathway and identifying novel AR-interacting partners, making it relevant for cancer research applications. -
Androgen Receptor Inhibitor
Faznolutamide is an androgen receptor inhibitor that interferes with androgen signaling. This compound exhibits significant antiandrogenic activity, making it a valuable tool for investigating androgen-dependent biological processes. It is used in research focused on prostate cancer and other conditions influenced by androgens. -
Androgen Receptor Inhibitor
Bifluranol is an androgen receptor inhibitor that functions by blocking the action of androgens, which are hormones that can promote the growth of certain cancers. This compound exhibits anti-androgenic activity, making it valuable in research addressing hormone-dependent cancers, such as prostate cancer. Bifluranol can be utilized in studies focused on understanding androgen signaling pathways and developing therapeutic strategies targeting androgen-related conditions. -
Androgen receptor Inhibitor
Androgen receptor-IN-5 is a potent inhibitor of the androgen receptor, demonstrating significant anticancer activity. This compound also disrupts the production of pro-inflammatory cytokines, including IL-17A, IL-17F, and IFN-γ, making it a valuable tool for studying androgen receptor signaling and its role in cancer and immune responses. Its multifaceted activity positions Androgen receptor-IN-5 as a promising candidate for research in cancer therapeutics and inflammation modulation. -
AR Degrader/CYP17A1 Inhibitor
YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context. -
AR/ARV7 Inhibitor
AR/AR-V7-IN-1 is a potent inhibitor of the androgen receptor (AR) and its splice variant AR-V7, with an IC50 of 172.85 nM. This compound effectively suppresses cell proliferation in LNCaP and 22RV1 cell lines, exhibiting IC50 values of 4.87 μM and 2.07 μM, respectively. Additionally, AR/AR-V7-IN-1 demonstrates significant tumor growth inhibition in 22RV1 xenograft models, making it a valuable tool for prostate cancer research. -
AR BF3 Inhibitor
VPC13163 is a potent inhibitor of the androgen receptor (AR) BF3 domain, exhibiting an IC50 value of 0.31 µM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in prostate cancer and other androgen-dependent malignancies. Its ability to selectively target the AR BF3 domain allows for the exploration of new therapeutic strategies in androgen receptor-mediated pathways. -
AR Inhibitor
AR Antagonist 6 is a diphenyl ether compound that acts as a selective androgen receptor (AR) antagonist, binding to the receptor with an affinity of 120 nM. This compound demonstrates low toxicity and shows promising in vitro activity in the golden Syrian hamster ear model. It serves as a valuable tool for research applications involving the modulation of androgen receptor signaling in various biological contexts. -
Androgen Receptor Inhibitor
Androgen receptor-IN-4 is a potent androgen receptor inhibitor that selectively targets the androgen receptor signaling pathway. This compound is particularly valuable for investigating the mechanisms underlying androgen-dependent conditions, including Kennedy's disease. Its application in research can contribute to a better understanding of therapeutic strategies for androgen receptor-related disorders. -
Androgen Receptor Inhibitor
AR Antagonist 2 is a potent inhibitor of the androgen receptor (AR), demonstrating an IC50 of 0.95 μM. This compound is crucial for cancer research, particularly in studies exploring androgen-driven pathways and potential therapeutic strategies in hormone-dependent malignancies. Its efficacy makes it a valuable tool for investigating AR-related biological mechanisms. -
Androgen Receptor Dimerization Inhibitor
M17-B15 is an androgen receptor dimerization inhibitor that demonstrates an IC50 of 30 nM. By effectively disrupting androgen receptor self-association, M17-B15 suppresses androgen receptor signaling pathways. This compound exhibits significant anti-prostate cancer efficacy in both in vitro studies and in mouse xenograft tumor models, making it a valuable tool for research in prostate cancer biology. -
Androgen Receptor Inhibitor
Androgen receptor-IN-3 is a selective inhibitor of the androgen receptor (AR), effectively reducing AR-driven transcriptional activity in LNCaP prostate cancer cells, with an IC50 of 5.04 μM. This compound is primarily utilized in research applications investigating androgen receptor signaling pathways and their role in prostate cancer progression. Its inhibitory effects on AR activity present a valuable tool for studying potential therapeutic strategies targeting androgen-dependent tumors. -
Androgen Receptor Inhibitor
Carbazole derivative 1 is an androgen receptor inhibitor that effectively reduces androgen and estrogen levels in mammals, including humans. This compound demonstrates significant potential in research applications focusing on hormone-related disorders and cancer treatments involving hormonal regulation. Its unique mechanism may provide insights into therapeutic strategies for managing conditions influenced by androgen and estrogen signaling pathways. -
Estrogen Receptor/ERR Inhibitor
Coumestrol is a phytoestrogen that targets the estrogen receptor, functioning as an ERR inhibitor. It demonstrates significant anti-proliferative activity against ES2 cells, with an IC50 value of 50 μM. Coumestrol is of interest in research related to cancer, neurological disorders, and autoimmune diseases due to its potential therapeutic effects. -
Viral Endonuclease Inhibitor
Licoflavone C is a viral endonuclease inhibitor with broad-spectrum antiviral activity. It exhibits estrogen-like properties and effectively inhibits the replication of various bunyaviruses, including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus, through a non-substrate competitive mechanism. Licoflavone C demonstrates an IC50 of 35.5 μM against SFTSV CEN, with a Kd of 9.53 μM. Additionally, it exhibits low cytotoxicity and genotoxicity while inducing apoptosis and alleviating chemotherapy-induced chromosomal damage. This compound is valuable for research on viral infections, particularly mechanisms related to severe fever with thrombocytopenia syndrome. -
Estrogen Receptor/ERR Inhibitor
α-Zearalenol is a mycotoxin that acts as an inhibitor of estrogen receptors (ER). As a derivative of zearalenone, it exhibits a high affinity for these receptors, leading to significant xenoestrogenic effects that can result in reproductive disorders in animals. This compound is utilized in research to study the impact of estrogenic exposure and its implications in endocrine disruption and reproductive health. -
Estrone Sulfatase Inhibitor
3-Formylsalicylic acid is a noncompetitive inhibitor of estrone sulfatase, displaying an IC50 value of 0.15 mM and a Ki value of 0.12 mM. This compound demonstrates low acute toxicity, making it a suitable candidate for research applications aimed at studying estrogen metabolism and related pathways in cancer biology. Its inhibitory effects on estrone sulfatase may provide insights into therapeutic strategies for hormone-dependent tumors. -
ERα Inhibitor
TPBM is a selective estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for the 17β-estradiol (E2)-ERα complex. This compound effectively diminishes the recruitment of E2·ERα to endogenous estrogen-responsive genes. Additionally, TPBM demonstrates the capacity to inhibit E2-dependent proliferation of ERα-positive cancer cells, exhibiting an IC50 of 5 μM. Notably, TPBM is non-toxic to normal cells and does not interfere with estrogen-independent cell growth, making it a valuable tool for research in hormone-responsive signaling pathways and cancer biology. -
Estrogen Receptor Inhibitor
Estrogen receptor-IN-1 is a potent inhibitor of the estrogen receptor (ER), demonstrating IC50 values of 13 µM for ERα and 5 µM for ERβ. This compound is utilized in research to investigate estrogen signaling pathways and the role of estrogen receptors in various biological processes, including cancer progression and hormone-related disorders. Its selective inhibition provides a valuable tool for studying ER function and therapeutic potential in related diseases. -
ERα Inhibitor
Fulvestrant-3-boronic acid is a potent estrogen receptor alpha (ERα) inhibitor that exhibits competitive binding with an IC50 of 4.1 nM. This compound effectively induces degradation of ERα in breast cancer cells, making it a valuable tool for research in estrogen receptor-related signaling pathways and breast cancer therapies. Its mechanism of action supports studies aimed at understanding ERα's role in tumor progression and treatment resistance. -
Estrogen Receptor/ERR Inhibitor
Elacestrant (S enantiomer) is a selective estrogen receptor (ERR) inhibitor known for its oral bioavailability. This compound exhibits differential inhibition with IC50 values of 48 nM for ERα and 870 nM for ERβ, demonstrating its potential as a targeted therapeutic agent in estrogen-related disorders. Its application in research includes studies focused on elucidating estrogen signaling pathways and developing treatments for hormone-responsive cancers. -
Estrogen Receptor/ERR Inhibitor
Elacestrant S enantiomer dihydrochloride is a selective estrogen receptor (ERR) inhibitor that targets the estrogen receptor with distinct pharmacological properties. This compound demonstrates reduced biological activity compared to its R enantiomer, offering potential applications in the study of estrogen signaling pathways. It serves as a valuable tool for researchers investigating the role of estrogen receptors in various biological processes and the development of therapies for estrogen receptor-positive cancers. -
Estrogen Receptor α Inhibitor
Raloxifene 6-Monomethyl Ether is a derivative of Raloxifene that selectively inhibits Estrogen Receptor α. This compound demonstrates significant biological activity, with an IC50 of 250 nM against MCF-7 breast cancer cells, leading to a pIC50 of 6.6. It is a valuable tool for research in hormone-dependent cancer studies and may provide insights into therapeutic strategies targeting estrogen signaling pathways.
