Pallesen, Jakob S. et al. published their research in Journal of Medicinal Chemistry in 2021 | CAS: 638-07-3

Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Recommanded Product: 638-07-3

Deconstructing Noncovalent Kelch-like ECH-Associated Protein 1 (Keap1) Inhibitors into Fragments to Reconstruct New Potent Compounds was written by Pallesen, Jakob S.;Narayanan, Dilip;Tran, Kim T.;Solbak, Sara M. Oe.;Marseglia, Giuseppe;Soerensen, Louis M. E.;Hoej, Lars J.;Munafo, Federico;Carmona, Rosa M. C.;Garcia, Anthony D.;Desu, Haritha L.;Brambilla, Roberta;Johansen, Tommy N.;Popowicz, Grzegorz M.;Sattler, Michael;Gajhede, Michael;Bach, Anders. And the article was included in Journal of Medicinal Chemistry in 2021.Recommanded Product: 638-07-3 The following contents are mentioned in the article:

Targeting the protein-protein interaction (PPI) between nuclear factor erythroid 2-related factor 2 (Nrf2) and Kelch-like ECH-associated protein 1 (Keap1) is a potential therapeutic strategy to control diseases involving oxidative stress. Here, six classes of known small-mol. Keap1-Nrf2 PPI inhibitors were dissected into 77 fragments in a fragment-based deconstruction reconstruction (FBDR) study and tested in four orthogonal assays. This gave 17 fragment hits of which six were shown by X-ray crystallog. to bind in the Keap1 Kelch binding pocket. Two hits were merged into pyrazole I with a 220-380-fold stronger affinity (Ki = 16μM) relative to the parent fragments. Systematic optimization resulted in several novel analogs with Ki values of 0.04-0.5μM, binding modes determined by X-ray crystallog., and enhanced microsomal stability. This demonstrates how FBDR can be used to find new fragment hits, elucidate important ligand-protein interactions, and identify new potent inhibitors of the Keap1-Nrf2 PPI. This study involved multiple reactions and reactants, such as Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3Recommanded Product: 638-07-3).

Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Organic chlorides can be used in production of: PVC, pesticides, chloromethane, teflon, insulators. Alkyl chlorides are versatile building blocks in organic chemistry. While alkyl bromides and iodides are more reactive, alkyl chlorides tend to be less expensive and more readily available.Recommanded Product: 638-07-3

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics