T6222

PFI-1 (PF-6405761), a specific BET (bromodomain-containing protein) inhibitor for BRD4, is with the IC50 of 0.22 μM in a cell-free assay.

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), an orally active NLRP3 inflammasome inhibitor, directly binds to its target with an IC50 of 1.23 μM for IL-1β inhibition. It demonstrates robust metabolic stability in liver microsomes (t1/2 = 138.63 min) and exhibits minimal toxicity (against L02: IC50 > 100 μM) [1].

α-Glucosidase-IN-11 is a highly permeable competitive inhibitor of α-glucosidase (IC50: 0.56 μM) that binds to the Trp residue in α-glucosidase, affecting protein folding and regulating blood glucose levels. [Topoisomerase II]

Topoisomerase IIα-IN-1 (compound 2) is a potent TopoIIα inhibitor and DNA-binding ligand, exhibiting significant anti-proliferative effects on human cancer cell lines.

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

Topoisomerase I inhibitor 8, a hexacyclic analogue of camptothecin, is also a potent inhibitor of topoisomerase I and is toxic to tumour cells.

Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual inhibitor of Dyrk1A and α-synuclein aggregation with an IC50 of 7.8 μM for α-synuclein. It exhibits high predictive CNS permeability and has a neuroprotective effect.

GP3269 is a selective, potent, orally active human adenosine kinase (AK) inhibitor (IC50: 11 nM) with anticonvulsant effects in rats.

KRAS G12D inhibitor 14 is a potent compound that binds the KRAS G12D protein (Kd: 33 nM) and selectively inhibits the active form KRAS G12D-GTP, but not KRAS G13D.

BBS-4 is a selective and potent inducible nitric oxide synthase (NOS2) dimerization inhibitor (IC50: 0.49 nM), and BBS-4 protects mice from the cardiovascular dysfunction of sepsis.