Activators & Inhibitors

POLA1 inhibitor 1 (Compound 12) is an orally active inhibitor of POLA1. POLA1 inhibitor 1 exhibits antitumour effects on several tumour tissue types and Adaroten-resistant cell lines.

TLR7/8 agonist 6 (Compound 4), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 0.18 and 5.34 μM for TLR7 and TLR8, respectively. TLR7/8 Antagonist

TLR7/8 Antagonist 1 (Compound 16c), an imidazoquinoline derivative, is a potent TLR7/8 agonist with IC50 values of 3.91 and 2.19 μM for TLR7 and TLR8, respectively. rel-O-2050 (TLR-2050) is a key target for drug development in infectious diseases, cancer and autoimmune diseases.

rel-O-2050 (Compound O-2050) is a neutral cannabinoid CB1receptor antagonist that reduces food intake in mice.

CB1/2 agonist 2 (compound 23) is a potent non-selective cannabinoid ligand with Ki of 3.5 nM and 1.2 nM, respectively. CB1/2 agonist 2 is a full agonist of CB1 and a competitive inverse agonist of CB2. BACE-IN-1 is a complete agonist of CB1 and a competitive inverse agonist of CB2.

BACE-IN-1 is an imidazo[1,2-a]pyridine derivative that inhibits the β-site amyloid precursor protein cleavage enzyme (BACE) sentence.BACE-IN-1 has the potential to investigate diseases involving BACE, such as Alzheimer's disease.

NIC-0102 is an orally active proteasome inhibitor (pIC50:7.55) that exhibits specific inhibition of NLRP3 inflammatory vesicle activation. Inhibitory effect.

IL-2-IN-1 is a potent inhibitor of IL-2 (IC50: 1978 nM) and exhibits anti-proliferative effects.

NRX-2663 is an enhancer of the interaction of β-catenin with the homologous E3 ligaseSCFβ-TrCP and has an enhanced effect on the binding of β-catenin to β-TrCP (Kd: 54.8 nM, EC50: 22.9 nM).