BLINK15 is a blood-brain barrier-permeable Cdk5 inhibitor. It reduces CDK5 activity in CDK5/p35 (IC50= 29.34 nM) and CDK5/p25 (IC50= 12.08 nM) complexes. Additionally, BLINK15 exhibits antidiabetic and neuroprotective effects. It lowers blood glucose levels in type 2 diabetes (T2D) mice, enhances cognitive abilities, and diminishes neurodegenerative lesions.

CDK9-CyclinT:74.63 nM

BLINK15, at a concentration of 50 nM to 100 nM for 24 hours, reduces CDK5 activity within CDK5/p35 (IC50 = 29.34 nM) and CDK5/p25 (IC50 = 12.08 nM) complexes. In N2A cell lines, overexpression of CDK5/p35 and CDK5/p25 leads to decreased CDK5 activity when treated with BLINK15 (50 nM-100 nM, 24 hours). Additionally, BLINK15 maintains over 50% cell viability across all doses in HEK293T, HepG2, and N2A cell lines at concentrations of 25-500 μM for 24 hours. BLINK15 also demonstrates the ability to penetrate the blood-brain barrier (BBB) and enter the central nervous system at concentrations of 100-500 μM over 7 hours.

BLINK15 (20-40 mg/kg/day, i.p., for 20 days) has shown potential in alleviating symptoms associated with type 2 diabetes in a mouse model fed a high-fat diet (HFD).