Description
Ph-HTBA a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain. Ph-HTBA showed enhanced mid-nanomolar affinity for the CaMKIIα binding site and a marked hub thermalstabilization effect along with a distinct CaMKIIα Trp403 flip upon binding. Moreover, Ph-HTBA has good cellular permeability and low microsomal clearance and shows brain permeability after systemic administration to mice, signified by a high Kp, uu value (0.85). Ph-HTBA is a promising candidate for CaMKIIα-associated pharmacological interventions and future clinical development.
Uses
Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders[1].
