For research use only. Not for therapeutic Use.
PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a Ki value of 490 nM[1][2].
PBD-150 is able to reduce the deposition of pyroglutamate-modified amyloid-β peptides in brain of transgenic mouse models of Alzheimer disease, leading to a significant improvement of learning and memory in those transgenic animals[3].
| Catalog Number | I017183 |
| CAS Number | 790663-33-1 |
| Synonyms | 1-(3,4-dimethoxyphenyl)-3-(3-imidazol-1-ylpropyl)thiourea |
| Molecular Formula | C15H20N4O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C15H20N4O2S/c1-20-13-5-4-12(10-14(13)21-2)18-15(22)17-6-3-8-19-9-7-16-11-19/h4-5,7,9-11H,3,6,8H2,1-2H3,(H2,17,18,22) |
| InChIKey | FZQXMGLQANXZRP-UHFFFAOYSA-N |
| SMILES | COC1=C(C=C(C=C1)NC(=S)NCCCN2C=CN=C2)OC |
| Reference | [1]. Buchholz M, et al. The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship. J Med Chem. 2006 Jan 26;49(2):664-77. [2]. DiPisa F, et al. The soluble Y115E-Y117E variant of human glutaminyl cyclase is a valid target for X-ray and NMR screening of inhibitors against Alzheimer disease. Acta Crystallogr F Struct Biol Commun. 2015 Aug;71(Pt 8):986-92. [3]. Huang KF, et al. Structures of human Golgi-resident glutaminyl cyclase and its complexes with inhibitors reveal a large loop movement upon inhibitor binding. J Biol Chem. 2011 Apr 8;286(14):12439-49. |
