ROR Inhibitor

ROR Inhibitors (22):

Cat. No.	Product Name	Effect	Purity

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 (K_d=1.13 μM).

HY-P99201

Zilovertamab	Inhibitor	98.20%
Zilovertamab (UC-961) is a humanised monoclonal antibody against ROR1 that blocks Wnt5a-induced ROR1 signalling.

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.

HY-169220S

RORγ/DHODH-IN-1	Inhibitor
RORγ/DHODH-IN-1 (compound 1404), a deuterium labeled compound, is a dual RORγ and DHODH inhibitor with IC₅₀ values of 9.7 nM and 100 nM, repaectively. RORγ/DHODH-IN-1 blocks the replication of SARS-CoV-2, HCMV, and non-enveloped DNA virus (HAdV5).

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.

HY-13421

SR1001	Inhibitor	99.89%
SR1001 is a selective ROR_α and ROR_γt inverse agonist with K_is 172 and 111 nM, respectively.

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]^.}

HY-137434

Cedirogant	Inhibitor	98.66%
Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.

HY-19774

GNE-0946	Inhibitor	98.09%
GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC₅₀ value of 4 nM for HEK-293 cell.

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 K_d of 380 nM.

HY-142296

RORγt inhibitor 1	Inhibitor
RORγt inhibitor 1 is a RORγt allosteric inhibitor with an IC₅₀ value of 1 nM.

HY-132195

RORγt inverse agonist 14	Inhibitor
RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC₅₀ of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis.

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.

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) .

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.

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.

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.

HY-142934

RORγt inhibitor 2	Inhibitor
RORγt inhibitor 2 (Compound 119) is a potent RORγt inhibitor with an IC₅₀ of 9.2 nM. RORγt inhibitor 2 can be used for the research of cancer, inflammation or autoimmune diseases mediated by RORγt.

HY-155487

JTE-151	Inhibitor
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.

HY-169222S

RORγ/DHODH-IN-2	Inhibitor
RORγ/DHODH-IN-2 (Compound 1311) is an orally active dual inhibitor of RORγ/DHODH with IC₅₀ values of 11.9 nM and 90 nM, respectively. RORγ/DHODH-IN-2 exhibits antiviral activity by inhibiting the activity of SARS-CoV-2, HCMV, HAdV5, and MPXV, with IC₅₀ values of 27 nM, 20 nM, 9.1 nM, and 1.8 nM, respectively.

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