ROR Inhibitor

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).

CS5001 Antibody is an IgG1 human monoclonal antibody targeting ROR1. CS5001 Antibody can be used for the synthesis of the ADC CS5001. It is applicable to research related to advanced solid tumors and lymphomas. The recommended isotype control is human IgG1 kappa (HY-P99001).

BL20-MMAE is an antibody-drug conjugate targeting ROR1, which is formed by conjugating an anti-ROR1 antibody with the Auristatin payload MMAE (HY-15162) via a BL20 linker.

huXBR1-402 (NBE-002 Antibody) is a high-affinity (K_d=5.8 nM) humanized chimeric rabbit/human monoclonal antibody that targets ROR1. huXBR1-402 specifically binds to the Ig/Fz domain epitope of human ROR1, directly inhibits the proliferation of ROR1-positive tumor cells and induces apoptosis of leukemia cells (apoptosis).

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.

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

ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor. ARI-1 blocks the PI3K/AKT/mTOR signaling pathway in a ROR1-dependent manner. ARI-1 upregulates cleaved-PARP and p-P38. ARI-1 induces Apoptosis. ARI-1 has anticancer activity against non-small cell lung cancer.

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

LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with K_i of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC₅₀ of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models.

Nebratamig (GNC-035) is an anti-ROR1/anti-CD3/anti-PD-L1/anti-4-1BB tetra-specific antibody with potential immunostimulatory and antineoplastic activities.

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.

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

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.

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.

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

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.

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

3-Oxo-5β-cholanoic acid (Standard) is the analytical standard of 3-Oxo-5β-cholanoic acid. This product is intended for research and analytical applications. 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)[1].

ROR1-IN-2 (compound 9I) is a potent and selective ROR1 inhibitor. ROR1-IN-2 exhibits antiproliferative activity in multiple cancer cells. ROR1-IN-2 significantly suppresses tumor growth in vivo.

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.