Development of Kinase Inactive PD173955 Analogues for Reducing Production of Aβ Peptides was written by Sinha, Anjana;Gindinova, Katherina;Mui, Emily;Netzer, William J.;Sinha, Subhash C.. And the article was included in ACS Medicinal Chemistry Letters in 2019.Recommanded Product: 171049-35-7 This article mentions the following:
Compound 3a, DV2-103, is a kinase inactive analog of a potent Abl1/Src kinase inhibitor, PD173955, 2. Both compounds, 2 and 3a, are known to reduce production of beta amyloid (Aβ) peptide in cells and animal models. We have now prepared and evaluated a series of PD-173955 analogs, several of which reduced Aβ production potently. This occurs in cells expressing human full-length amyloid precursor protein (APP) and not in cells expressing APP β-C terminal fragment (APP-C99), suggesting that the kinase inactive analogs strongly affect β-secretase (BACE1) cleavage of APP, similarly to Gleevec. A combination of the kinase inactive analogs of PD173955 with a BACE1 inhibitor (BACEi), namely BACE IV, strongly reduced Aβ levels in cells, as noted previously with Gleevec and analogs. Several potent compounds also penetrated and accumulated in mouse brain in high nanomolar to low micromolar concentration In the experiment, the researchers used many compounds, for example, tert-Butyl [4,4′-bipiperidine]-1-carboxylate (cas: 171049-35-7Recommanded Product: 171049-35-7).
tert-Butyl [4,4′-bipiperidine]-1-carboxylate (cas: 171049-35-7) belongs to piperidine derivatives. The piperidine ring can be found not only in more than half of the currently known structures of alkaloids, but also in many natural or synthetic compounds with interesting biological activities. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Recommanded Product: 171049-35-7
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem