Activators & Inhibitors

Tubulin polymerization-IN-9 is a potent inhibitor of tubulin (IC50: 1.82 μM). Tubulin polymerization-IN-9 arrests the cell cycle of K562 cells in G2/M phase and induces apoptosis and mitochondrial depolarization. Tubulin polymerization-IN-9 exhibits potent anti-vascular and anti-tumour effects.

Parapenzolate bromide is an orally active mAChR antagonist. parapenzolate bromide is an anticholinergic and antitussive agent.

NN-390 is a selective, potent HDAC6 inhibitor (IC50: 9.8 μM) that crosses the blood-brain barrier. nN-390 has potential for studies in metastatic group 3 neural tube cell tumours.

DGAT1-IN-3 is a selective, potent, orally active DGAT-1 inhibitor that inhibits human DGAT-1 (IC50: 38 nM) and rat DGAT-1 (IC50: 120 nM).DGAT1-IN-3 can be used in studies of obesity, dyslipidemia and metabolic syndrome.

NLRP3-IN-8 (compound 27) is an orally active, directly binding NLRP3 inflammasome inhibitor with an IC 50 value of 1.23 μM against IL-1 β. NLRP3-IN-8 has good metabolic stability to liver microsomes (t 1/2 = 138.63 min), and has almost no toxicity (against L02: IC 50 > 100 μM) [1] .

α-Glucosidase-IN-11 is a highly permeable competitive inhibitor of α-glucosidase (IC50: 0.56 μM). α-Glucosidase-IN-11 binds to the Trp residue in α-glucosidase and has a regulatory effect on protein folding and can be used for the regulation of blood glucose levels. Topoisomerase II

Topoisomerase IIα-IN-1 (compound 2) is a DNA-binding ligands and a potent inhibitor of TopoIIα, a topoisomerase. topoisomerase IIα-IN-1 shows good anti-proliferative effects on human cancer cell lines.

Topoisomerase IIα-IN-2 (compound 5) is a DNA-binding ligands and a potent inhibitor of the topoisomerase TopoIIα. Topoisomerase IIα-IN-2 exhibits high anti-proliferative activity in human cancer cell lines. Topoisomerase IIα-IN-2 arrests the cell cycle of cancer cells in the G2/M phase and significantly induces DNA damage.

Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual inhibitor of Dyrk1A and α-synuclein aggregation that acts on α-synuclein (IC50: 7.8 μM). Dyrk1A/α-synuclein-IN-2 has a high predictive CNS permeability and neuroprotective effect.