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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.
Synonyms: VTP-43742
AGN-242428, also known as VTP-43742, is a potent, selective and orally active RORγt inhibitor for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis.
S18-000003 is a potent orally bioavailable retinoic acid receptor-related orphan receptor-gamma-t (RORγt) inhibitor with an IC50 of 29 nM. S18-000003 inhibits IL-17 production.
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.
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.
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Synonyms: IMU-935
Izumerogant (IMU-935) is an orally active dual inhibitor of RORγ and DHODH, with IC50 values of 10 nM and 98 nM, respectively. This compound effectively disrupts the replication of various viruses, including SARS-CoV-2, HCMV, and HAdV5, demonstrated by EC50 values ranging from 3.6 to 17 nM. Izumerogant serves as a valuable tool for investigating antiviral mechanisms and therapeutic strategies against viral infections.
RORγ/DHODH-IN-2 is a potent dual inhibitor of RORγ and DHODH, exhibiting IC50 values of 11.9 nM and 90 nM, respectively. This compound demonstrates significant antiviral activity against multiple viruses, including SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC50 values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively. RORγ/DHODH-IN-2 is ideal for research applications targeting immune signaling pathways and viral infections.
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RORγt/DHODH-IN-1 is a dual inhibitor targeting retinoic acid receptor-related orphan receptor gamma t (RORγt) and dihydroorotate dehydrogenase (DHODH). With IC50 values of 0.083 μM for RORγt and 0.172 μM for DHODH, this compound demonstrates significant potency. RORγt/DHODH-IN-1 has been shown to possess notable in vivo anti-inflammatory activity, making it a valuable tool for research in immunology and inflammation-related studies.
RORγt/DHODH-IN-3 is a dual inhibitor targeting both RORγt and dihydroorotate dehydrogenase (DHODH), exhibiting IC50 values of 0.098 μM for RORγt and 0.432 μM for DHODH. This compound demonstrates significant in vivo anti-inflammatory activity, making it a valuable tool for researchers investigating autoimmune diseases and other inflammatory conditions. Its dual mechanism of action positions it as a promising candidate for therapeutic development in these areas.
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RORγt/DHODH-IN-2 is a potent dual inhibitor of RORγt and DHODH, targeting key pathways involved in immune regulation and inflammation. This compound exhibits significant biological activity that can be leveraged in the investigation of inflammatory bowel disease (IBD) and related immune disorders. Its dual action provides a valuable tool for research into therapeutic strategies aimed at modulating RORγt and DHODH activity in inflammatory contexts.
Synonyms: Dehydrolithocholic acid; 3-oxoLCA
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.
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.
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.
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.
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 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.
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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-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.
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CID 7309015 is a selective inhibitor of retinoic acid-related orphan receptor gamma (ROR-γ). This compound demonstrates significant potential in modulating inflammatory pathways, particularly in the context of NF-κB signaling and inflammatory arthritis research. CID 7309015 serves as a valuable tool for investigating the roles of ROR-γ in immune response and inflammatory diseases.
RORγt inhibitor 3 is a potent and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), which plays a crucial role in Th17 cell differentiation. This compound demonstrates high binding affinity and effectively modulates immune responses, making it particularly relevant for research in autoimmune disorders. Its efficacy has been validated in mouse models of experimental autoimmune encephalomyelitis (EAE) and collagen-induced arthritis (CIA), highlighting its potential for therapeutic applications in inflammatory diseases.
