Catalog No.
Product Name
Application
Product Information
Citations
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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. -
RORγt Inverse Agonist
RORγt inverse agonist 13 is a selective inverse agonist targeting the RORγt receptor with an IC50 of 63.8 nM. This compound demonstrates potent biological activity, making it suitable for research applications focusing on autoimmune diseases and T cell differentiation. Its improved agent-like properties enhance its utility in preclinical studies investigating the modulation of RORγt signaling pathways. -
RORγ Inverse Agonist
SR1555 is a specific inverse agonist of the retinoic acid receptor-related orphan nuclear receptor γ (RORγ), exhibiting an IC50 value of 1 μM. This compound is known to effectively inhibit TH17 cell development and function while promoting an increase in T regulatory cell frequency and downregulating IL-17 expression. SR1555 is valuable for investigating mechanisms in autoimmune disease research. -
RORγ Antagonist
(±)-ML 209 is a selective RORγ antagonist that effectively inhibits RORγt transcriptional activity, demonstrating an IC50 of 300 nM in HEK293t cells. This diphenylpropanamide compound specifically suppresses murine Th17 cell differentiation while leaving the differentiation of naïve CD4+ T cells into Th1 and regulatory T cell lineages unaffected. Its unique mechanism makes (±)-ML 209 a valuable tool for researchers investigating the role of RORγ in immune responses and related diseases. -
RORγt Activator
7ß,27-Dihydroxycholesterol (7β, 27-OHC) is a selective activator of RORγt, exhibiting a Ki of 120 nM. This compound plays a crucial role in promoting the differentiation of CD4+ Th17 cells in both mouse and human models. Additionally, 7ß,27-Dihydroxycholesterol enhances IL-17 production through a CYP27A1-dependent pathway, making it valuable for studies focused on immune response and related signaling pathways. -
RORγt Inverse Agonist
Cedirogant is an orally active inverse agonist of the retinoic acid receptor-related orphan receptor gamma-t (RORγt). It demonstrates significant potential in modulating immune responses, particularly in the context of psoriasis research. This compound serves as a valuable tool for investigating therapeutic strategies targeting autoimmune and inflammatory conditions. -
RORγt Antagonist
TMP920 is a potent and selective antagonist of RORγt, a retinoic acid receptor-related orphan receptor involved in immune signaling. It effectively inhibits the binding of RORγt to the SRC1 peptide, demonstrating an IC50 value of 0.03 μM. TMP920 is valuable for research applications focusing on autoimmune diseases, as well as the modulation of Th17 cell differentiation and function. -
ROR Antagonist
GNE-3500 is a selective, orally active antagonist of Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3), exhibiting an EC50 of 12 nM. This compound demonstrates favorable pharmacokinetic properties in rat models, making it a valuable tool for research applications focused on modulating RORc-related pathways. GNE-3500 is particularly relevant for studies investigating autoimmune diseases and inflammatory responses where RORc plays a critical regulatory role. -
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 Inverse Agonist
RORγt Inverse Agonist 10 is a potent inverse agonist targeting the retinoic acid receptor-related orphan nuclear receptor gamma t (RORγt), with an IC50 of 51 nM. This compound effectively suppresses the expression of key genes involved in the pathogenesis of psoriasis, including IL-17A, IL-22, and IL-23R. It is suitable for research applications exploring the mechanisms of autoimmune diseases and the development of novel therapeutics for psoriasis. -
ROR Agonist
RORγt inverse agonist 23 is a potent and selective inverse agonist targeting the retinoic acid receptor-related orphan receptor gamma t (RORγt). This compound demonstrates significant biological activity as an immunomodulator, making it valuable in the investigation of autoimmune diseases and inflammatory disorders. Its oral bioavailability enhances its utility in preclinical studies and therapeutic research applications. -
RORγt Agonist
RORγt Agonist 3 is a potent activator of RORγt, crucial for the differentiation of Th17 cells. This compound enhances the production of pro-inflammatory cytokines, thereby boosting lymphocyte cytotoxicity. Additionally, RORγt Agonist 3 suppresses the generation of regulatory T cells, which may lead to an augmented immune response, making it valuable for research into immune modulation and inflammatory diseases. -
RORγ(t) Agonist
Hexyl 4-hydroxybenzoate, also known as Hexylparaben, is a selective agonist for the retinoic acid-related orphan receptor RORγ(t), exhibiting an EC50 value of 144 nM. This compound is valuable in the investigation of autoimmune diseases and immune-related processes, providing insights into the modulation of immune responses and potential therapeutic interventions. Its role in RORγ(t) signaling makes it a crucial tool for researchers studying T-cell differentiation and related pathways. -
ROR1 Ligand
Antitumor agent-127 is a macrocyclic peptide that targets the ROR1 receptor. It exhibits nanomolar affinity for ROR1, demonstrating effective binding and substantial internalization in 786-O and MDA-MB-231 tumor cell lines. This compound is valuable for research in cancer biology, particularly in studies focused on ROR1-mediated signaling pathways and potential therapeutic applications in tumors expressing ROR1. -
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. -
ROR Agonist
RORγt agonist 1 is a potent agonist of the RORγt receptor, demonstrating an EC50 of 20.8 nM. This compound exhibits high metabolic stability, enhanced aqueous solubility, and favorable pharmacokinetics in murine models. RORγt agonist 1 is a promising candidate for cancer immunotherapy research applications, targeting immune modulation pathways to aid in therapeutic strategies. -
RORγ Antagonist
Retezorogant is a selective antagonist of the retinoid-related orphan receptor gamma (RORγ). This compound plays a significant role in modulating immune responses and has potential applications in the treatment of autoimmune diseases and inflammatory conditions. Retezorogant's ability to inhibit RORγ activity makes it a valuable tool for researchers investigating the mechanisms of Th17 cell differentiation and related pathways. -
ROR Agonist
RORγ Agonist 1 is a potent agonist of the RORγ nuclear receptor, exhibiting an EC50 of 21 nM. This compound demonstrates significant antitumor activity, making it a valuable tool in cancer research. Its oral bioavailability facilitates convenient administration in preclinical studies exploring RORγ's role in tumor progression and immune modulation. -
RORγt Inverse Agonist
RORγt inverse agonist 14 is a selective inverse agonist targeting the retinoic acid receptor-related orphan receptor gamma t (RORγt) with an EC50 of 2.5 nM. This compound exhibits significant anti-inflammatory properties, making it suitable for research into autoimmune conditions such as rheumatoid arthritis and psoriasis. Its oral bioavailability facilitates in vivo studies, contributing valuable insights into RORγt modulation in therapeutic contexts. -
RORγt Inverse Agonist
RORγt Inverse Agonist 6 is designed to inhibit the RORγt receptor, a key regulator in Th17-driven autoimmune diseases. This compound effectively suppresses IL-17A gene expression following IL-23 stimulation in vivo, making it a valuable tool for exploring therapeutic strategies against inflammatory conditions. Its application is essential for researchers investigating the role of Th17 cells in various autoimmune disorders. -
RORγt Inverse Agonist
FM26 is a potent allosteric inverse agonist of the retinoic acid receptor-related orphan receptor γt (RORγt), exhibiting an IC50 of 264 nM. This compound effectively downregulates IL-17a mRNA expression in EL4 cells, making it a valuable tool for studying Th17 cell differentiation and related immunological responses. FM26 is suitable for research applications focusing on autoimmune diseases and inflammation. -
ROR Antagonist
RORγt Inverse Agonist 3 is a selective and orally bioavailable inverse agonist of RORγ, exhibiting potent activity with EC50 values of 0.22 μM for human RORγ and 0.15 μM for RORγt in human IL-17 cells. This compound is useful for investigations into the regulation of immune responses and the role of RORγt in inflammatory diseases. Its ability to inhibit RORγt activity makes it a valuable tool for research into conditions such as autoimmune disorders and cancer. -
RORγt Inverse Agonist
RORγt inverse agonist 26 is a potent inverse agonist of the RORγt receptor, crucial for modulating Th17 cell differentiation. This compound effectively inhibits the production of interleukin-17 (IL-17), making it valuable for research into inflammation and autoimmune disorders. Delving into RORγt functionality, this reagent is instrumental in therapeutic development and understanding immune system regulation. -
RORγ inverse agonist
ARN-6039 is an orally active inverse agonist of RORγ, a transcription factor involved in the regulation of various immune responses. This compound demonstrates potential in modulating immune activity and may be effective in the treatment of autoimmune demyelinating diseases. It serves as a valuable tool for research aimed at understanding the role of RORγ in immune-related disorders and developing therapeutic strategies targeting these conditions. -
ROR Modulator
SHR168442 is a selective modulator of retinoid-related orphan receptor gamma (RORγ), exhibiting an IC50 value of 0.035 μM. This compound significantly influences RORγ activity, making it valuable for research applications related to immune response and inflammatory diseases. Its precise modulation of RORγ provides insights into pathways regulated by this receptor, facilitating studies in cellular signaling and potential therapeutic interventions. -
RORγt Inverse Agonist
RORγt Inverse Agonist 8 acts as a selective inverse agonist targeting the retinoic acid receptor-related orphan receptor gamma t (RORγt). With an IC50 of 19 nM for the human RORγt ligand-binding domain, this compound demonstrates significant potential in modulating RORγt activity. Its biological activity is relevant for research in autoimmune diseases and T helper 17 (Th17) cell differentiation, providing a valuable tool for investigators studying immune response pathways. -
RORγt Modulator
RORγt modulator 5 is a selective modulator of the RORγt nuclear receptor, exhibiting a Ki value of less than 100 nM. This compound has demonstrated potential in the study of inflammatory, metabolic, and autoimmune diseases that are mediated by RORγt. Its ability to influence RORγt signaling pathways makes it a valuable tool for researchers investigating these disease mechanisms. -
RORγ antagonist
RORγ antagonist 1 is a potent antagonist of the retinoic acid receptor-related orphan receptor gamma (RORγ) with a dissociation constant (KD) of 0.18 μM. This compound demonstrates significant anti-proliferative effects in HPAF-II pancreatic cancer xenograft models. Additionally, RORγ antagonist 1 inhibits key signaling pathways, including RAS/MAPK and AKT/mTORC1, and induces caspase-dependent apoptosis in pancreatic cancer cells, making it a valuable tool for cancer research and potential therapeutic applications. -
RORγt Inverse Agonist
TMP780 is an inverse agonist of the nuclear receptor RORγt, demonstrating an IC50 value of 13 nM. This compound exhibits potential for modulating immune responses and inflammation, making it a valuable tool for research related to cutaneous inflammatory disorders. Its ability to inhibit RORγt activity positions TMP780 as a promising candidate for studies aimed at uncovering therapeutic strategies in inflammatory diseases. -
RORγt Agonist
RORγt Agonist 2 is a selective agonist of the Retinoic acid receptor-related orphan receptor gamma t (RORγt), which plays a critical role in the differentiation of Th17 cells. This compound enhances the production of pro-inflammatory cytokines, thereby increasing lymphocyte cytotoxicity. Additionally, RORγt Agonist 2 inhibits the generation of regulatory T cells, ultimately promoting a more robust immune response. Its applications include research in autoimmune diseases and immunotherapy. -
RORγt Modulator
RORγt modulator 2 is a selective modulator of retinoid-related orphan receptor γt (RORγt), exhibiting an IC50 of less than 50 nM. This compound is valuable for investigating RORγt-mediated pathologies including pain, inflammation, chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative disorders, and cancer. Research on RORγt modulator 2 can contribute to understanding therapeutic approaches targeting these conditions. -
RORγt Inverse Agonist
RORγt inverse agonist 28 is a potent inverse agonist targeting the retinoic acid receptor-related orphan receptor gamma t (RORγt). It effectively regulates the differentiation of T helper 17 (Th17) cells and inhibits interleukin-17 (IL-17) production. This compound is valuable for research into inflammation and autoimmune diseases, providing insights into potential therapeutic approaches. -
RORγt Modulator
RORγt modulator 4 is an effective modulator of the RORγt pathway. It has been shown to influence IL-17A production in cells derived from mouse spleen, thereby contributing to research in autoimmune diseases and inflammation. This compound is valuable for studies aimed at understanding the role of RORγt in T cell differentiation and related biological processes. -
RORγ Inverse Agonist
RORγ inverse agonist 2 is a potent inverse agonist targeting the retinoic acid receptor-related orphan receptor RORγ, exhibiting IC50 values of 0.4 μM and 0.9 μM for Gal4-RORγ and full-length RORγ, respectively. This compound is significant for research applications focused on autoimmune diseases, providing insights into RORγ's role in immune regulation and pathology. -
RORγ Inverse Agonist
JNJ-54119936 is an inverse agonist of the retinoic acid receptor-related orphan receptor gamma (RORγ) with a Kd of 5.3 nM. This compound exhibits significant modulation of RORγ activity, making it valuable for research into autoimmune diseases and inflammatory responses. Its specific targeting of RORγ allows for the exploration of downstream signaling pathways and therapeutic applications in related biological processes. -
RORγt Modulator
RORγt Modulator 3 is a selective modulator of the retinoic acid receptor-related orphan receptor gamma t (RORγt). This compound exhibits significant biological activity in the modulation of immune responses, making it valuable for research into RORγt-mediated diseases, including pain, inflammation, chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative disorders, and various cancer types. Its application may facilitate the development of novel therapeutic strategies targeting RORγt pathways. -
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 Reverse Agonist
TF-S14 is a reverse agonist of RORγt, a transcription factor critically involved in Th17 cell differentiation and cytokine production. By binding to RORγt, TF-S14 effectively inhibits the secretion of pro-inflammatory cytokines such as IL-17A, IL-21, and IL-22. This compound is valuable for research applications focused on autoimmune diseases and transplantation rejection mechanisms. -
RORγt Inverse Agonist
RORγt inverse agonist 34 is a selective inverse agonist of the retinoic acid receptor-related orphan receptor gamma t (RORγt), exhibiting an IC50 of 0.094 μM for the RORγt-LBD. This compound demonstrates significant biological activity in modulating RORγt signaling pathways, making it a valuable tool for research into psoriasis and related inflammatory conditions. Its use facilitates the exploration of therapeutic strategies targeting RORγt in the regulation of immune responses. -
RORγt Agonist
RORγt Agonist 4 is a potent and selective agonist of the retinoic acid receptor-related orphan receptor gamma t (RORγt). This compound enhances metabolic stability and demonstrates significant biological activity in preclinical models. Notably, RORγt Agonist 4 has shown therapeutic potential in tumor models, including mouse B16F10 melanoma and LLC lung adenocarcinoma, making it a valuable tool for investigating RORγt-mediated pathways in cancer research. -
RORγt Inverse Agonist
RORγt Inverse Agonist 32 is an orally active compound that targets the RORγt receptor as an inverse agonist. It plays a critical role in modulating inflammatory pathways and is valuable for research into immune responses and related diseases. This compound is particularly useful for studies focusing on the regulation of Th17 cell differentiation and the development of autoimmune conditions. -
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. -
RORα Agonist
Gala-SR (Gala-SR1078) is a selective RORα agonist that enhances the amplitude of circadian rhythms, making it a valuable tool for the investigation of disorders related to circadian regulation. This compound has potential applications in studying rhythm disturbances and can provide insights into the role of circadian mechanisms in periodontitis research. Its ability to modulate rhythmic activity positions it as a significant reagent in the exploration of chronobiology and its implications for human health. -
RORγ Inverse Agonist
CD12681 is a selective inverse agonist of RORγ, exhibiting IC50 values of 19 nM and 10 nM against RORγ GAL4 and CD4-IL-17 cells, respectively. This compound effectively reduces IL-17-mediated inflammatory cell recruitment, making it a valuable tool for studying inflammatory pathways. CD12681 shows promise for research applications in conditions such as psoriasis, facilitating the exploration of novel therapeutic strategies. -
RORγ Antagonist
SR1555 hydrochloride is a selective inverse agonist of the retinoic acid receptor-related orphan nuclear receptor γ (RORγ), exhibiting an IC50 of 1 μM. This compound effectively inhibits the development and function of pro-inflammatory TH17 cells while promoting an increase in anti-inflammatory T regulatory (Treg) cells. SR1555 hydrochloride is primarily utilized in research targeting autoimmune diseases, providing insights into potential therapeutic strategies for immune modulation. -
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.
