1351761-44-8 Usage
Uses
Different sources of media describe the Uses of 1351761-44-8 differently. You can refer to the following data:
1. Leucine-rich repeat kinase 2 (LRRK2) is an enzyme that interacts with parkin, a ligase that is part of the ubiquitin-proteasome system that mediates the targeting of proteins for degradation. Loss of function of the parkin protein leads to dopaminergic cell death. The development of Parkinson's disease has been strongly associated with mutations in the LRRK2 gene that lead to increased kinase activity. GNE-7915 is a selective, brain-penetrable LRRK2 inhibitor (Kis = 2 and 18.7 nM in biochemical and cell-based assays, respectively). It inhibits LRRK2 Ser1292 autophosphorylation in BAC transgenic mice expressing human LRRK2 protein with the G2019S Parkinson’s disease mutation with an IC50 value of 20 nM in vivo.[Cayman Chemical]
2. GNE-7915 is a Blood-Brain Barrier (BBB) penetrable small molecule inhibitor of Leucine-Rich Repeat Kinase 2 (LRRK2).
Check Digit Verification of cas no
The CAS Registry Mumber 1351761-44-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,3,5,1,7,6 and 1 respectively; the second part has 2 digits, 4 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1351761-44:
(9*1)+(8*3)+(7*5)+(6*1)+(5*7)+(4*6)+(3*1)+(2*4)+(1*4)=148
148 % 10 = 8
So 1351761-44-8 is a valid CAS Registry Number.
1351761-44-8Relevant articles and documents
The tale of proteolysis targeting chimeras (PROTACs) for Leucine-Rich Repeat Kinase 2 (LRRK2)
Konstantinidou, Markella,Oun, Asmaa,Pathak, Pragya,Zhang, Bidong,Wang, Zefeng,ter Brake, Frans,Dolga, Amalia M.,Kortholt, Arjan,D?mling, Alexander
, p. 959 - 965 (2020/12/30)
Here we present the rational design and synthetic methodologies towards proteolysis-targeting chimeras (PROTACs) for the recently-emerged target leucine-rich repeat kinase 2 (LRRK2). Two highly potent, selective, brain-penetrating kinase inhibitors were selected, and their structure was appropriately modified to assemble a cereblon-targeting PROTAC. Biological data show strong kinase inhibition and the ability of the synthesized compounds to enter the cells. However, data regarding the degradation of the target protein are inconclusive. The reasons for the inefficient degradation of the target are further discussed.
AMINOPYRIMIDINE DERIVATIVES AS LRRK2 INHIBITORS
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Page/Page column 72, (2011/12/14)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compound
