Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC AR degrader
ARD-61 is a highly potent and selective PROTAC degrader of the androgen receptor (AR), also capable of degrading progesterone receptors (PR) in AR-positive cancer cell lines. It induces apoptosis and demonstrates significant antitumor efficacy in vivo, effectively inhibiting tumor growth in the MDA-MB-453 xenograft mouse model. Additionally, ARD-61 is equipped with an alkyne functional group, enabling its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules, facilitating conjugation and functionalization for chemical biology applications. -
PROTAC ERα Degrader
PROTAC ERα Degrader-1 is a bifunctional molecule composed of an estrogen receptor-alpha (ERα) ligand, a linker, and an E3 ubiquitin ligase-recruiting moiety. Derived from compound P1 in patent WO2017201449A1, it functions as a targeted protein degrader that promotes ubiquitination and subsequent proteasomal degradation of ERα. PROTAC ERα Degrader-1 represents a novel approach for modulating estrogen receptor signaling in hormone-dependent cancers. -
PROTAC AR Degrader
ARD-2128 is a highly potent, orally bioavailable PROTAC degrader targeting the androgen receptor (AR). It efficiently reduces AR protein levels, downregulates AR-regulated gene expression in tumor tissues, and inhibits tumor growth without observable toxicity. ARD-2128 is a promising tool for prostate cancer research. -
PROTAC AR-V7 degrader
MTX-23 is an androgen receptor (AR)-targeting PROTAC that degrades both AR-FL and the splice variant AR-V7. It effectively inhibits prostate cancer cell proliferation and induces apoptosis, making it a promising tool for studying AR signaling and therapeutic resistance in prostate cancer. -
androgen receptor (AR) PROTAC degrader
BMS-986365 (CC-94676) is an orally active, selective PROTAC degrader targeting the androgen receptor (AR), including AR mutants. It functions via cereblon (CRBN)-mediated ubiquitination and proteasomal degradation of AR. BMS-986365 exhibits strong in vivo efficacy by suppressing AR signaling and inhibiting tumor growth in advanced prostate cancer models, making it a promising candidate for therapeutic development. -
estrogen receptor PROTAC protein degrader
Vepdegestrant (ARV-471) is an orally bioavailable PROTAC designed to target and degrade the estrogen receptor (ER). It is being developed for the treatment of patients with locally advanced or metastatic ER+/HER2− breast cancer, offering a novel approach to overcome endocrine resistance through targeted ER degradation. -
androgen receptor (AR) PROTAC degrader
Bavdegalutamide (ARV-110) is an orally active and highly specific PROTAC degrader targeting the androgen receptor (AR). It induces ubiquitination and proteasomal degradation of AR, offering a novel therapeutic approach for AR-driven diseases such as prostate cancer. -
Androgen Receptor (AR) degrader
ARCC-4 is a low-nanomolar PROTAC degrader targeting the androgen receptor (AR), with a DC₅₀ of 5 nM. Based on enzalutamide and incorporating a von Hippel-Lindau (VHL) E3 ligase ligand, ARCC-4 efficiently degrades both wild-type and clinically relevant AR mutants linked to resistance to antiandrogen therapy. It outperforms enzalutamide in potency and degradation efficacy, making it a promising candidate for advanced prostate cancer research. -
PROTAC Androgen Receptor Degrader
ARD-266 is a potent PROTAC degrader targeting the Androgen Receptor (AR) through a von Hippel-Lindau E3 ligase mechanism. It effectively induces AR protein degradation in AR-positive prostate cancer cell lines, including LNCaP, VCaP, and 22Rv1, with DC50 values ranging from 0.2 to 1 nM. Additionally, ARD-266 features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating versatile applications in chemical biology research. -
GPR18 Agonist
N-Arachidonylglycine (NA-Gly) selectively acts as an agonist for the GPR18 receptor, exhibiting an EC50 value of 44.5 nM. Unlike its structural analog anandamide, NA-Gly does not engage with CB1 or CB2 receptors. This compound also demonstrates inhibitory activity on GLYT2 with an IC50 of 5.1 μM. Additionally, N-Arachidonylglycine has been shown to effectively promote the migration of endometrial cells, making it a valuable tool for research in cellular migration and cannabinoid receptor activity. -
PROTAC ERRα Degrader
PROTAC ERRα Degrader-3 is a selective degrader targeting estrogen-related receptor alpha (ERRα) through a von Hippel-Lindau-based mechanism. This compound effectively induces the degradation of ERRα protein by over 80% at a concentration of 30 nM, while showing no activity against ERRβ and ERRγ. It serves as a valuable tool for researchers investigating the role of ERRα in various biological processes and disease states. -
PROTAC AR Degrader
ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand. -
Glucocorticoid Receptor Activator
Glucocorticoid Receptor Activator 1 is a phenyl aziridine precursor that selectively activates the glucocorticoid receptor (GR). This compound down-regulates TNF-induced pro-inflammatory gene expression, making it a valuable tool for studying inflammation mechanisms. Its role in modulating inflammatory responses positions it as an important reagent for research in various inflammatory conditions. -
Human Endogenous Metabolite
Estradiol (β-Estradiol) is a steroid hormone and the major female sex hormone. Estradiol can up-regulate the expression of neural markers of human endometrial stem cells (hEnSCs) and promote their neural differentiation. Estradiol can be used for the research of cancers, neurodegenerative diseases and neural tissue engineering. -
Endogenous Glucocorticoids
Corticosterone (17-Deoxycortisol) is an orally active and adrenal cortex-produced glucocorticoid, which plays an important role in regulating neuronal functions of the limbic system (including hippocampus, prefrontal cortex, and amygdala). Corticosterone increases the Rab-mediated AMPAR membrane traffic via SGK-induced phosphorylation of GDI. Corticosterone also interferes with the maturation of dendritic cells and shows a good immunosuppressive effect. -
TIGIT/PVR Blocker
Liothyronine is an active form of thyroid hormone that primarily targets thyroid hormone receptors TRα and TRβ. It exhibits binding affinities of 2.33 nM and 2.29 nM for human TRα and TRβ, respectively. In addition, Liothyronine binds to PVR and effectively inhibits the interaction between TIGIT and PVR. This compound is useful in research applications related to thyroid hormone signaling and immune modulation studies. -
GnRH Antagonist
Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist that effectively inhibits the endogenous luteinizing hormone surge during ovarian stimulation. This compound is utilized in research to study its role in reproductive processes, particularly in the modulation of ovarian function. Additionally, Cetrorelix has demonstrated the ability to reduce cyclophosphamide-induced ovarian follicular destruction in animal models, making it invaluable for studies related to ovarian preservation and fertility. -
GR Agonist
Flumethasone is a highly selective and potent glucocorticoid receptor (GR) agonist. It effectively activates GR, leading to the inhibition of nuclear factor kappa B (NF-κB) and subsequent reduction of pro-inflammatory cytokine production, such as TNF-α and IL-1β. Additionally, Flumethasone upregulates anti-inflammatory gene expression, particularly IL-10, and modulates metabolic enzyme activity, including tyrosine aminotransferase. This compound is valuable for research into inflammatory diseases, cancer, and endocrine regulation. -
LHRH Analogue
[D-Lys6]-LH-RH is a potent analogue of Luteinizing-hormone-releasing hormone (LHRH) that acts as a GnRH receptor agonist. This compound demonstrates significant activity in promoting the release of luteinizing hormone, making it valuable for endocrine research. Its applications extend to studies focused on reproductive biology, fertility treatments, and hormone regulation. -
Estrogen receptor agonist
4,4'-Sulfonyldiphenol, an estrogen receptor agonist, is a significant chemical interest due to its role as a substitute for Bisphenol A in various industrial and consumer applications. This compound exhibits competitive binding to thyroid hormone receptors with IC50 values of 2650 μM for TRα and 2294 μM for TRβ, influencing breast development and androgen receptor downregulation in fetal testes. Additionally, 4,4'-Sulfonyldiphenol promotes glioblastoma progression by activating the EZH2-mediated PI3K/AKT/mTOR pathway. Chronic exposure can lead to lipid accumulation and metabolic alterations, including dyslipidemia and obesity, while also inducing intestinal inflammation through microbiome disruption and accelerating atherosclerosis in zebrafish models. -
ERα PRRTAC Degrader
GNE-5472 is a potent bifunctional degrader targeting estrogen receptor alpha (ERα) through the PRRTAC mechanism. By functioning as a pan-IAP antagonist, GNE-5472 inhibits cIAP1/2, thereby activating the non-classical NF-κB pathway, which leads to significant upregulation of TNFα expression. This compound effectively inhibits the proliferation of breast cancer cells and promotes apoptosis. GNE-5472 is valuable for research applications in the study of breast cancer and related signaling pathways. -
hTNFa Antibody-GC Conjugate
Glucocorticoid receptor agonist-4 Ala-Ala-Mal is a conjugate of an anti-human TNFα antibody and a glucocorticoid receptor agonist. This compound is designed to selectively target and activate glucocorticoid receptors, demonstrating significant anti-inflammatory properties. It is primarily utilized in research focused on autoimmune and inflammatory diseases, enabling in-depth studies of immune response modulation and therapeutic interventions. -
MRGPRX2 Antagonist
GE1111 is an antagonist of the MRGPRX2 receptor, with an IC50 value of 9.4 μM. This compound effectively inhibits MRGPRX2/MRGPRB2-mediated mast cell activation, leading to the reduction of pro-inflammatory cytokines, including TSLP, IL-13, MCP-1, TNF-α, and IL-1β. Additionally, GE1111 preserves claudin 1 and involucrin expression, enhances macrophage phagocytic activity, and modulates STIM1 and phosphorylated AKT activation. Its anti-inflammatory and anti-allergic properties make GE1111 relevant for research in conditions such as rosacea, atopic dermatitis, and ulcerative colitis. -
hTNFa Antibody-GC Conjugate
Glucocorticoid receptor agonist-3 Ala-Ala-Mal is a conjugate of a human TNFα antibody and a glucocorticoid receptor agonist. This compound is designed to modulate the immune response, exhibiting anti-inflammatory properties that are relevant in the study of autoimmune and inflammatory diseases. Its application offers valuable insights into therapeutic strategies targeting TNFα, enhancing the understanding of its role in various pathological conditions. -
GPRC5D/CD3ε/TNFRSF17 Antibody
Ramantamig is a humanized monoclonal antibody that targets CD3ε on T cells, as well as GPRC5D and TNFRSF17 (BCMA) on multiple myeloma cells. It facilitates T-cell-mediated cytotoxicity by forming immunological synapses, leading to selective killing of myeloma cells without non-specific T-cell activation when target cells are absent. Additionally, Ramantamig has been engineered to minimize interactions with Fc receptors, enhancing its specificity. This reagent is ideal for research in multiple myeloma therapies. -
Glucocorticoid Receptor Agonist
Amcinonide is a glucocorticoid receptor agonist that exhibits anti-inflammatory properties by inhibiting nitric oxide (NO) release with an IC50 of 3.38 nM. It effectively downregulates the expression of pro-inflammatory genes such as iNOS, TNF-α, and IL-1β in glial cells. Moreover, Amcinonide alters T cell populations by reducing T6+/Ia+ cells while increasing T6+/Ia- cells, leading to a selective decrease in Ia antigen expression. This compound is applicable in research related to eczematous dermatitis and the modulation of inflammatory responses. -
HDAC
Estrogen Receptor β/HDAC Probe 1 is a near-infrared fluorescent probe designed to simultaneously target the estrogen receptor β and histone deacetylase (HDAC). This probe enables the study of dynamic interactions between these two critical proteins, facilitating the investigation of their roles in cellular signaling and gene regulation. It is particularly useful in cancer research and other studies involving estrogen signaling pathways and epigenetic modifications. -
GPR68 Inhibitor
Ogremorphin is a selective inhibitor of the G protein-coupled receptor GPR68. This compound exhibits notable anti-inflammatory and anti-tumor properties, demonstrating the ability to inhibit the migration of human melanoma cells and induce ferroptosis in glioblastoma cells. Ogremorphin is a valuable tool for researchers investigating the roles of GPR68 in cancer biology and inflammation. -
Estrogen Receptor/ERR Inhibitor
Estradiol cypionate is a 17β-cypionate ester of estradiol that acts as a selective estrogen receptor modulator. It functions by inhibiting the synthesis of endothelin-1 (ET-1), a key factor in vascular biology. This compound is widely utilized in research exploring estrogenic effects, hormonal signaling pathways, and the therapeutic potential of estrogen receptor modulation in various physiological and pathological conditions. -
EGFR Inhibitor, Estrogen Receptor Inhibitor, Progesterone Receptor Inhibitor
4,7-Dihydroxycoumarin is a potent inhibitor of the epidermal growth factor receptor (EGFR) as well as estrogen and progesterone receptors. It exhibits significant cytotoxicity against breast cancer cells, with an IC50 value of 18.36 μg/mL. This compound is valuable for research focused on breast cancer treatment and the exploration of hormone receptor interactions. -
Glucocorticoid Receptor Agonist
Fluocinolone (Acetonide) is a glucocorticoid receptor agonist that exhibits significant anti-inflammatory and anti-lipid accumulation effects. It promotes the proliferation of dermal papilla cells (DPCs) and shows potential in the repair of injured pulp tissues. This compound is also valuable in research focused on mitigating chemotherapy-induced peripheral neuropathy associated with Paclitaxel. -
SHRs Agonist
Triamcinolone is a long-acting corticosteroid that acts as a glucocorticoid receptor agonist. It exhibits multiple biological activities, including anti-inflammatory, anti-oedematous, anti-proliferative, anti-angiogenic, immunomodulatory, and neuroprotective effects. This compound is widely utilized in research for the treatment of various dermatological conditions, immune disorders, and ocular diseases. -
ERα Antagonist
ERα antagonist 1 is a selective covalent antagonist of estrogen receptor α (ERα). It has demonstrated the ability to induce apoptosis and arrest the cell cycle in the G0/G1 phase in MCF-7 breast cancer cells. This compound is valuable for research focused on understanding estrogen signaling pathways and the development of targeted therapies for ERα-positive tumors. -
RORγ Inhibitor
W6134 is a potent and selective covalent inhibitor of RORγ, displaying an IC50 of 0.21 μM. This compound demonstrates remarkable selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 effectively suppresses RORγ transcriptional activity and has been shown to inhibit proliferation and colony formation while inducing apoptosis in castration-resistant prostate cancer (CRPC) cells. It is a valuable tool for investigating the mechanisms and treatment strategies for CRPC. -
GnRHR Antagonist
Degarelix acetate hydrate is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist. This compound effectively inhibits the GnRH signaling pathway, making it a valuable tool in prostate cancer research. It is used to study the modulation of hormone levels and the impact on tumor growth dynamics. -
ERα Degrader
OBHSA is a selective estrogen receptor alpha (ERα) degrader that facilitates the degradation of cyclin D1, effectively bypassing resistance to Tamoxifen. By inducing an increase in intracellular reactive oxygen species, OBHSA activates the unfolded protein response (UPR) excessively, leading to apoptosis in susceptible cells. Additionally, OBHSA serves as an ERα ligand for the synthesis of PROTAC degraders, making it a valuable tool in the study of ERα-mediated pathways and therapeutic resistance in cancer research. -
Anticancer Agent/Immune Modulator/GPR120 Activator
Phytosphingosine is a bioactive sphingolipid that functions primarily as an immunomodulator and activator of GPR120. Exhibiting anti-inflammatory, antibacterial, and anticancer properties, Phytosphingosine can induce apoptosis in various cell types. Its role in regulating immune responses makes it a valuable reagent for research on inflammatory skin diseases and type II diabetes. Additionally, with an IC50 value of 33.4 μM, Phytosphingosine enhances understanding of GPR120-mediated pathways. -
Mineralocorticoid/Glucocorticoid Receptor Agonist
Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. It exhibits significant anti-inflammatory properties by suppressing pro-inflammatory cytokine expression, including CCL2, IL-6, and IL-8 levels, while enhancing renal sodium and water transport, which contributes to increased plasma volume and blood pressure. Additionally, fludrocortisone induces key signaling pathways such as PI3K/Akt, mTOR, and ERK1/2, and is utilized in research applications related to congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency. -
ER Modulator
MPP hydrochloride is a potent selective modulator of the estrogen receptor (ER). It has been shown to induce significant apoptosis in endometrial cancer and oLE cell lines while antagonizing the positive effects of beta-estradiol. In vivo studies reveal its mixed agonist/antagonist activity on murine uterine ERalpha, making it a valuable tool for research into estrogen-related pathways and cancer therapeutics. -
Androgen Receptor Inhibitor
SC428 is a selective androgen receptor (AR) inhibitor that targets the N-terminal domain, effectively reducing the transactivation of various isoforms including AR-V7, AR-v567es, and full-length AR (AR-FL) along with its LBD mutants. This compound inhibits the nuclear translocation, chromatin binding, and subsequent transcription of AR-regulated genes in response to androgens. Additionally, SC428 demonstrates significant anti-proliferative effects on tumor cells in vitro and promotes apoptosis in vivo, particularly in mice bearing 22RV1 xenografts. Its application in cancer research highlights its potential utility in targeting androgen-dependent tumors. -
Androgen Receptor PROTAC Degrader
PROTAC AR Degrader-8 is an androgen receptor (AR) PROTAC degrader that effectively induces degradation of full-length AR (AR-FL) with DC50 values of 0.018 μM in 22Rv1 cells and 0.14 μM in LNCaP cells, as well as degrading the AR-V7 variant with a DC50 of 0.026 μM in 22Rv1 cells. This compound exhibits potent inhibition of cancer cell proliferation, with IC50 values of 0.038 μM and 1.11 μM in 22Rv1 and LNCaP cells, respectively. PROTAC AR Degrader-8 induces G2/M cell cycle arrest and promotes apoptosis in 22Rv1 cells, demonstrating significant anticancer efficacy in both murine and zebrafish models. It is a valuable tool for investigating mechanisms underlying prostate cancer and castration-resistant prostate cancer. -
ERα/ERβ AModulator
Ferutinin, a natural terpenoid compound, modulates estrogen receptors ERα and ERβ, acting as an agonist with an IC50 of 33.1 nM for ERα and exhibiting antagonist properties with an IC50 of 180.5 nM for ERβ. This compound enhances calcium permeability in lipid bilayer membranes and mitochondria, functioning as an electrogenic Ca2+-ionophore. Ferutinin displays a range of biological activities including estrogenic, antitumor, antibacterial, and anti-inflammatory effects, making it a valuable tool for research in cancer biology, hormonal regulation, and inflammation pathways. -
PROTAC ERα Degrader
PROTAC ERα Degrader-4 is a selective degrader targeting estrogen receptor alpha (ERα) through the PROTAC mechanism. It exhibits potent inhibitory activity with a Ki value of 5.08 μM, effectively leading to the degradation of ERα in both Tamoxifen-sensitive and resistant ER+ breast cancer cells, as well as in ERα-mutated breast cancer cell lines. Additionally, PROTAC ERα Degrader-4 induces apoptosis, making it a valuable tool for cancer research aimed at understanding and combating ERα-driven malignancies. -
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. -
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.
