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-163192
    W6134
    Inhibitor 99.90%
    W6134 is highly potent and selective RORγ covalent inhibitor with IC50 of 0.21 μM. W6134 exhibits superior activity ini nhibiting the proliferation and colony formation and inducing apoptosis. W6134 can be used for the research of cancer.
    W6134
  • HY-142940
    RORγt modulator 5
    Modulator
    RORγt modulator 5 is a RORγt modulator with a Ki value of <100 nM. RORγt modulator 5 has the potential for inflammatory, metabolic, autoimmune and other diseases mediated by RORy study (WO2017132432A1; compound 2).
    RORγt modulator 5
  • HY-155542
    RORγ antagonist 1
    Antagonist
    RORγ antagonist 1 (compound 22), a potent betulinic acid derivative, is an antagonist of RORγ (KD=0.18 μM). RORγ antagonist 1 exhibits anti-proliferative activity in HPAF-II pancreatic cancer xenograft model. RORγ antagonist 1 inhibits RAS/MAPK and AKT/mTORC1 pathway, and induces caspase-dependent apoptosis in pancreatic cancer cells.
    RORγ antagonist 1
  • HY-102075B
    TMP780
    Antagonist 99.51%
    TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable agent target for the treatment of cutaneous inflammatory disorders.
    TMP780
  • HY-163612
    XY077
    Agonist
    XY077 (compound 14a) is a RORγ inverse agonist with the IC50 of 0.004 μM. XY077 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro.
    XY077
  • HY-142937
    RORγt agonist 2
    Agonist
    RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17).
    RORγt agonist 2
  • HY-142843
    RORγt/DHODH-IN-1
    Inhibitor
    RORγt/DHODH-IN-1 (compound (R)-14d) is a potent and orally active dual RORγt/DHODH inhibitor, with IC50s of 0.083 μM and 0.172 μM, respectively. RORγt/DHODH-IN-1 exhibits remarkable in vivo anti-inflammatory activity.
    RORγt/DHODH-IN-1
  • HY-142935
    RORγt modulator 2
    Modulator
    RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphan receptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
    RORγt modulator 2
  • HY-100084
    Methyl-3β-hydroxycholenate
    Modulator
    Methyl-3β-hydroxycholenate is a ROR gamma modulator extracted from patent US20110263046 A1, in figure 2.
    Methyl-3β-hydroxycholenate
  • HY-142703
    RORγt inverse agonist 28
    Inhibitor
    RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .
    RORγt inverse agonist 28
  • HY-142939
    RORγt modulator 4
    Modulator
    RORγt modulator 4 is a RORγt modulator. RORγt modulator 4 has an activity to modulate IL-17A production in cells derived from mouse spleen (WO2018030550A1; compound 146).
    RORγt modulator 4
  • HY-142847
    RORγt/DHODH-IN-3
    Inhibitor
    RORγt/DHODH-IN-3 (compound (S)-14d) is a dual RORγt/DHODH inhibitor, with IC50s of 0.098 μM and 0.432 μM, respectively. RORγt/DHODH-IN-3 exhibits remarkable in vivo anti-inflammatory activity.
    RORγt/DHODH-IN-3
  • HY-142834
    RORγt/DHODH-IN-2
    Inhibitor
    RORγt/DHODH-IN-2 (compound 1) is a potent dual RORγt/DHODH inhibitor. RORγt/DHODH-IN-2 can be used for inflammatory bowel disease (IBD) research.
    RORγt/DHODH-IN-2
  • HY-148237
    JNJ-54119936
    Antagonist
    JNJ-54119936 is a novel RORγ (RORc) inverse agonist (Kd=5.3 nM).
    JNJ-54119936
  • HY-142936
    RORγt modulator 3
    Modulator
    RORγt modulator 3 (Compound 23) is a modulator of retinoid-related orphan receptor γt (RORγt). RORγt modulator 3 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
    RORγt modulator 3
  • HY-162490
    TF-S14
    Inhibitor
    TF-S14 is a reverse agonist of RORγt. TF-S14 reduces Th17 cell-associated cytokine production, including IL-17A, IL-21, and IL-22 by binding to and inhibiting RORγt activity. TF-S14 can be used in the study of autoimmune diseases and rejection in allotransplantation.
    TF-S14
  • HY-163611
    XY039
    Agonist
    XY039 (compound 13e) is a RORγ inverse agonist with the IC50 of 0.55 μM. XY039 induces cell apoptosis and shows antiproliferative activity in vivoand in vitro.
    XY039
  • HY-126037
    (±)-ML 209
    Antagonist 99.87%
    (±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4+ T cells into other lineages, including Th1 and regulatory T cells.
    (±)-ML 209
  • HY-155548
    RORγt inverse agonist 31
    Inhibitor
    RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. RORγt inverse agonist 31 can alleviate the severity of Imiquimod (HY-B0180)-induced psoriasis in mice.
    RORγt inverse agonist 31
  • HY-160021
    RORγt agonist 4
    Agonist
    RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma.
    RORγt agonist 4
Cat. No. Product Name / Synonyms Application Reactivity

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