1. Signaling Pathways
  2. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  3. ROR

ROR

RAR-related orphan receptor

Retinoic acid receptor-related orphan receptors (RORs) are a subfamily of the thyroid hormone receptor, which is a subfamily of the nuclear receptors and belonging to the orphan nuclear receptor family. The ROR subfamily contains three members: RORα (NR1F1), RORβ (NR1F2), and RORγ (NR1F3) and function as ligand-dependent transcription factors.

RORs are reported to activate transcription through ligand-dependent interactions with co-regulators and are involved in the development of secondary lymphoid tissues, autoimmune diseases, inflammatory diseases, the circadian rhythm, and metabolism homeostasis.

RORα and RORγ are important regulators of the immune system. The development and differentiation of Th17 cells are dependent on these factors. RORγ is expressed in lymphoid tissue inducer cells, innate lymphoid cells, invariant natural killer T cells, and γδ T cells, which contribute to inflammation and autoimmune disease.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-135319
    Strictinin
    Inhibitor
    Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1.
    Strictinin
  • HY-137434
    Cedirogant
    Inhibitor 98.66%
    Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.
    Cedirogant
  • HY-131338
    RORγt inverse agonist 13
    Inhibitor 98.13%
    RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC50 of 63.8 nM.
    RORγt inverse agonist 13
  • HY-117819
    TMP920
    Antagonist 99.92%
    TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
    TMP920
  • HY-120785
    SR1555
    Antagonist 99.69%
    SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases.
    SR1555
  • HY-16983
    GNE-3500
    Antagonist 98.90%
    GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats.
    GNE-3500
  • HY-155487
    JTE-151
    Inhibitor 99.34%
    JTE-151 is a RORγ inhibitor, which can suppress overactive immune response through inhibition of RORγ related to the activation of Th17 cells, making JTE-151 possible to be used in autoimmune disease research.
    JTE-151
  • HY-103637A
    Vimirogant hydrochloride
    Inhibitor 98.39%
    Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant hydrochloride exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant hydrochloride inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant hydrochloride has the potential for autoimmune disorders research.
    Vimirogant hydrochloride
  • HY-128604
    XY101
    Inhibitor 99.65%
    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
    XY101
  • HY-133552
    RORγt Inverse agonist 10
    Antagonist 99.13%
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
    RORγt Inverse agonist 10
  • HY-119366
    S18-000003
    Inhibitor 99.31%
    S18-000003 is a potent, selective and orally active inhibitor of retinoic acid receptor-related orphan receptor-gamma-t (RORγt), with an IC50 of <30 nM towards human RORγt in competitive binding assays. S18-000003 shows selectivity for RORγt over other ROR family members (IC50>10 μM). S18-000003 can be used for the research of psoriasis with low risk of thymic aberrations.
    S18-000003
  • HY-139847
    RORγt inverse agonist 23
    Agonist 99.34%
    RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
    RORγt inverse agonist 23
  • HY-142938
    RORγt agonist 3
    Agonist 98.12%
    RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23).
    RORγt agonist 3
  • HY-RS12132
    RORC Human Pre-designed siRNA Set A
    Inhibitor

    RORC Human Pre-designed siRNA Set A contains three designed siRNAs for RORC gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    RORC Human Pre-designed siRNA Set A
  • HY-W150866
    Hexyl 4-hydroxybenzoate
    Agonist 99.83%
    Hexyl 4-hydroxybenzoate (Hexylparaben) is a retinoic acid-related orphan receptor RORγ(t) agonist with an EC50 of 144 nM. Hexyl 4-hydroxybenzoate is used in the study of autoimmune diseases.
    Hexyl 4-hydroxybenzoate
  • HY-161096
    Antitumor agent-127
    99.09%
    Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines.
    Antitumor agent-127
  • HY-402601
    Desethyl-SID 7969543
    Control 98.83%
    Desethyl-SID 7969543 is an isoquinolinone analog of SID 7969543 (HY-107404) and a selective SF-1 (NR5A1) inhibitor. Desethyl-SID 7969543 shows no activity against RORA, VP16 and LRH-1, and exhibits no cytotoxicity at concentrations close to its SF-1 IC50 value.
    Desethyl-SID 7969543
  • HY-136527
    BMS-986251
    Antagonist
    BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
    BMS-986251
  • HY-142296
    RORγt inhibitor 1
    Inhibitor
    RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC50 value of 1 nM.
    RORγt inhibitor 1
  • HY-163192
    W6134
    Inhibitor 99.90%
    W6134 is highly potent and selective RORγ covalent inhibitor with an IC50 of 0.21 μM. W6134 exhibits excellent selectivity for RORγ over RORα, RXRγ, and ERRγ. W6134 significantly inhibits RORγ transcriptional activity W6134 inhibits the proliferation and colony formation and induces apoptosis in castration-resistant prostate cancer cells (CRPC). W6134 can be used for the research of castration-resistant prostate cancers (CRPC).
    W6134
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