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ROR modulators target retinoic acid receptor-related orphan receptors (RORs), a family of nuclear receptors. The family has three members, RORα, RORβ and RORγ, which bind ROR response elements in target genes and are active without an added ligand. RORα contributes to circadian clock regulation, and the immune isoform RORγt directs the differentiation of interleukin-17 (IL-17)-producing T helper (Th17) cells. In 2011 the synthetic RORα/γ ligand SR1001 was shown to suppress Th17 differentiation and autoimmunity in mice. SR-2211 and XY101 act on RORγ, whereas SR3335 is selective for RORα. SR1078 is used as an agonist of RORα and RORγ in studies of target gene expression. Related receptors without well-defined ligands are listed under Orphan Nuclear Receptor.
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.
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.
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 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.
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 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.
Synonyms: Hexylparaben
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.
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.
Synonyms: VTP-43742 hydrochloride
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.
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 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.
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.
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 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 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.
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.
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 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.
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.
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 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 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 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.
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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 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.
