Activators & Inhibitors

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).

GABA-AT-IN-1 (Compound 6) is an inhibitor of γ-aminobutyric acid transaminase (GABA-AT) that crosses the blood-brain barrier.

ART615 is a related isomer of ART558. ART615 inhibits Polθ by <10% at 12 μM and is able to act as a control for ART558 (IC50:7.9 nM).

CSF1R-IN-6 is a potent inhibitor of CSF1R. CSF1R-IN-6 is a potent inhibitor of CSF1R, which is expressed in macrophages and is dependent on the CSF-1/CSF-1R signalling pathway for survival and differentiation of macrophages. Compound 5).

PIM1-IN-6 (compound 5h) is a potent inhibitor of PIM-1 (IC50: 0.60 μM).PIM1-IN-6 has a high cytotoxic effect on HCT-116 and MCF-7 cells with IC50 values of 1.51 and 15.2 μM, respectively.