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

ROR

RAR-related orphan receptor

ROR

Related Products

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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.

ROR Isoform Specific Products:

ROR Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10626
    T0901317
    		Antagonist 99.93%
    T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
    T0901317
  • HY-N0155
    Nobiletin
    		Agonist 99.52%
    Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
    Nobiletin
  • HY-14422
    SR1078
    		Agonist 99.46%
    SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.
    SR1078
  • HY-125801
    3-Oxo-5β-cholanoic acid
    		Inhibitor 99.37%
    3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
    3-Oxo-5β-cholanoic acid
  • HY-P99201
    Zilovertamab
    		Inhibitor 98.20%
    Zilovertamab (UC-961) is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling.
    Zilovertamab
  • 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-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-14413
    SR3335
    		Antagonist 98.06%
    SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
    SR3335
  • HY-12776
    GSK805
    		Inhibitor 98.01%
    GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity.
    GSK805
  • HY-13421
    SR1001
    		Inhibitor 99.89%
    SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
    SR1001
  • HY-104037
    Cintirorgon
    		Agonist 98.53%
    Cintirorgon (LYC-55716) is a first-in-class, selective and orally bioavailable RORγ agonist. Cintirorgon (LYC-55716) modulates gene expression of RORγ expressing T lymphocyte immune cells, resulting in enhanced effector function, as well as decreased immunosuppression, resulting in decreased tumor growth, and improved survival.
    Cintirorgon
  • HY-16998
    SR2211
    		Antagonist 99.67%
    SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
    SR2211
  • HY-120210
    XY018
    		Antagonist 99.90%
    XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD).
    XY018
  • HY-N2253
    Neoruscogenin
    		Agonist 99.24%
    Neoruscogenin, a member of the steroidal sapogenin family, is a high-affinity agonist of the nuclear receptor RORα (NR1F1) (EC50 = 0.11 µM).
    Neoruscogenin
  • HY-101454
    SR0987
    		Agonist 99.65%
    SR0987, a SR1078 analog, is a RORγt agonist, with an EC50 of 800 nM. SR0987 increases IL17 expression while repressing the expression of PD-1.
    SR0987
  • HY-139534
    ARI-1
    		Inhibitor 99.76%
    ARI-1 is an inhibitor of receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 effectively inhibits aberrant ROR1 expression, which is associated with the development of non-small cell lung cancer (NSCLC) and EGFR-TKI-induced drug resistance. ARI-1 binds to the extracellular Frizzled domain of ROR1 and regulates PI3K/AKT/mTOR signaling in a ROR1-dependent manner. ARI-1 potently inhibits NSCLC cell proliferation and migration and has antitumor activity in vivo[1].
    ARI-1
  • HY-19770
    GSK2981278
    		Antagonist 99.51%
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding.
    GSK2981278
  • HY-139780
    JNJ-61803534
    		Inhibitor 99.88%
    JNJ-61803534 is a potent and orally active RORγt inverse agonist with an IC50 of 9.6  nM. JNJ-61803534 has anti-inflammatory activity. JNJ-61803534 inhibits IL-17A production in human CD4+ T cells under Th17 differentiation conditions.
    JNJ-61803534
  • HY-19775
    GNE-6468
    		Antagonist 98.04%
    GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC.
    GNE-6468
Cat. No. Product Name / Synonyms Application Reactivity
ROR Isoform Comparison

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