Category: 884494-51-3

Cawood, Emma E. published the artcileModulation of amyloidogenic protein self-assembly using tethered small molecules, Recommanded Product: 2-Fluoro-4-iodonicotinic acid, the main research area is amyloidogenic protein self assembly intermediate structure tethered small mol; human beta 2 microglobulin variant aggregation intermediate structure.

Protein-protein interactions (PPIs) are involved in many of life’s essential biol. functions yet are also an underlying cause of several human diseases, including amyloidosis. The modulation of PPIs presents opportunities to gain mechanistic insights into amyloid assembly, particularly through the use of methods which can trap specific intermediates for detailed study. Such information can also provide a starting point for drug discovery. Here, we demonstrate that covalently tethered small mol. fragments can be used to stabilize specific oligomers during amyloid fibril formation, facilitating the structural characterization of these assembly intermediates. We exemplify the power of covalent tethering using the naturally occurring truncated variant (ΔN6) of the human protein β2-microglobulin (β2m), which assembles into amyloid fibrils associated with dialysis-related amyloidosis. Using this approach, we have trapped tetramers formed by ΔN6 under conditions which would normally lead to fibril formation and found that the degree of tetramer stabilization depends on the site of the covalent tether and the nature of the protein-fragment interaction. The covalent protein-ligand linkage enabled structural characterization of these trapped, off-pathway oligomers using X-ray crystallog. and NMR, providing insight into why tetramer stabilization inhibits amyloid assembly. Our findings highlight the power of “”post-translational chem. modification”” as a tool to study biol. mol. mechanisms.

Journal of the American Chemical Society published new progress about Amyloid fibril. 884494-51-3 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodonicotinic acid, and the molecular formula is C6H3FINO2, Recommanded Product: 2-Fluoro-4-iodonicotinic acid.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Pierre, Romain published the artcileNovel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature, SDS of cas: 884494-51-3, the main research area is disubstituted pyridinone preparation kinase inhibitor; 7-azabenzotriazole; hinge-binder; ionic hydrogenation; library; pyridine-2(1H)-one.

A novel complementary multiparallel synthetic routes permitting the exploitation of the C-3 then C-4 vectors or vice versa to deliver library of novel 3,4-disubstituted pyridin-2(1H)-one kinase inhibitors I [R = (CH2)3OCH3, Ph, 2-EtC6H4, etc.; R1 = 4-NH2C6H10, CH2C(Me)2CH2NH2, cyclohexyl, etc.; R2 = H; R1R2 = CH2CH2OCH2CH2] starting from readily-available 2-chloro-4-fluoronicotinic acid and 2-fluoro-4-iodonicotinic acid resp. was developed. Perhaps the highlight of library route development was the novel transformation to the desired pyridin-2(1H)-one motif via in situ formation of the C2-OAt ether during HATU coupling and its cleavage under ionic hydrogenation conditions at just room temperature

Beilstein Journal of Organic Chemistry published new progress about Enzyme inhibitors (kinase). 884494-51-3 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodonicotinic acid, and the molecular formula is C6H3FINO2, SDS of cas: 884494-51-3.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Pierre, Romain published the artcileNovel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature, SDS of cas: 884494-51-3, the main research area is disubstituted pyridinone preparation kinase inhibitor; 7-azabenzotriazole; hinge-binder; ionic hydrogenation; library; pyridine-2(1H)-one.

A novel complementary multiparallel synthetic routes permitting the exploitation of the C-3 then C-4 vectors or vice versa to deliver library of novel 3,4-disubstituted pyridin-2(1H)-one kinase inhibitors I [R = (CH2)3OCH3, Ph, 2-EtC6H4, etc.; R1 = 4-NH2C6H10, CH2C(Me)2CH2NH2, cyclohexyl, etc.; R2 = H; R1R2 = CH2CH2OCH2CH2] starting from readily-available 2-chloro-4-fluoronicotinic acid and 2-fluoro-4-iodonicotinic acid resp. was developed. Perhaps the highlight of library route development was the novel transformation to the desired pyridin-2(1H)-one motif via in situ formation of the C2-OAt ether during HATU coupling and its cleavage under ionic hydrogenation conditions at just room temperature

Beilstein Journal of Organic Chemistry published new progress about Enzyme inhibitors (kinase). 884494-51-3 belongs to class iodides-buliding-blocks, name is 2-Fluoro-4-iodonicotinic acid, and the molecular formula is C6H3FINO2, SDS of cas: 884494-51-3.

Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com