| Bioactivity | 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]. |
| Target | Kd: 757 nM (CaMKIIα) |
| Invitro | Ph-HTBA can inhibit HOCPCA binding with a Ki value of 1.4 μM[1].Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM[1].Ph-HTBA (compound 1i) has a marked hub thermal stabilization effect along with a distinct CaMKIIα Trp403 flip upon binding[1]. |
| In Vivo | Ph-HTBA has good cellular permeability and low microsomal clearance and shows brain permeability after systemic administration to mice[1]. |
| Name | Ph-HTBA |
| CAS | 2368927-41-5 |
| Formula | C19H18O3 |
| Molar Mass | 294.34 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Yongsong Tian,et al. Exploring the NCS-382 Scaffold for CaMKIIα Modulation: Synthesis, Biochemical Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain. J Med Chem. 2022 Nov 8. |