ROR Inhibitor

ROR Inhibitors (24):

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-12776

GSK805	Inhibitor	98.26%
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-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-163192

W6134	Inhibitor
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.

HY-P99201

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

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-137434

Cedirogant	Inhibitor	99.41%
Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research.

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.

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.

HY-103637A

Vimirogant hydrochloride	Inhibitor	98.39%
Vimirogant (VTP-43742) hydrochloride is a potent, selective, and orally active RORγt inhibitor (K_i=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.

HY-128604

XY101	Inhibitor	98.88%
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-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.

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-126252

A-9758	Inhibitor
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC₅₀=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.

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.

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