| Bioactivity | PBD-150 is a human glutaminyl cyclase (hQC) Y115E-Y117E variant inhibitor, with a Ki value of 490 nM[1][2]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | PBD-150 | ||||||||||||
| CAS | 790663-33-1 | ||||||||||||
| Formula | C15H20N4O2S | ||||||||||||
| Molar Mass | 320.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |