264131-80-8

Upstream product

• 37993-32-1 1-amino-cyclohexanecarboxylic acid methyl ester hydrochloride 
• 155689-53-5 1-((S)-2-Benzyloxycarbonylamino-3-phenyl-propionylamino)-cyclohexanecarboxylic acid methyl ester 
• 221303-31-7 1-[(S)-2-Acetylamino-3-(4-chloromethyl-phenyl)-propionylamino]-cyclohexanecarboxylic acid methyl ester 
• 221303-30-6 Ac-Phe-Ac₆c-OMe 
• 46276-89-5 3-(5-methyl-indol-1-yl)-propylamine 
• 18210-83-8 3-(5-Methylindol-1-yl)propionitrile 
• 614-96-0 5-methyl-1H-indole 
• 1161-13-3 N-Cbz-L-Phe 
• 13086-84-5 di-tert-butyl phosphite 
• 264131-78-4 {4-[2-(1-{2-carbamoyl-1-[3-(5-methyl-indol-1-yl)-propylcarbamoyl]-ethylcarbamoyl}-cyclohexylcarbamoyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)-ethyl]-benzyl}-phosphonic acid di-tert-butyl ester 
• 264131-76-2 (1-{2-carbamoyl-1-[3-(5-methyl-indol-1-yl)-propylcarbamoyl]-ethylcarbamoyl}-cyclohexyl)-carbamic acid 9H-fluoren-9-ylmethyl ester 
• 264131-77-3 2-[(1-amino-cyclohexanecarbonyl)-amino]-N¹-[3-(5-methyl-indol-1-yl)-propyl]-succinamide 
• 162648-54-6 1-[((9H-fluoren-9-yl)methoxy)carbonylamino]cyclohexanecarboxylic acid 
• 166409-77-4 L-N_α-(9-fluorenylmethoxycarbonyloxy)-4-[(di-tert-butyl)phosphonomethyl]phenylalanine 

Relevant academic research and scientific papers

Inhibition of Grb2 SH2 domain binding by non-phosphate-containing ligands. 2. 4-(2-Malonyl)phenylalanine as a potent phosphotyrosyl mimetic

Nonhydrolyzable phosphotyrosyl (pTyr) mimetics serve as important components of many competitive Grb2 SH2 domain inhibitors. To date, the most potent of these inhibitors have relied on phosphonate-based structures to replace the 4-phosphoryl group of the

Highly potent inhibitors of the Grb2-SH2 domain

Highly potent inhibitors of the Grb2-SH2 domain have been synthesized. They share the common sequence: Ac-Pmp-Ac6c-Asn-NH-(3-indolyl-propyl). Different substituents at the 3-indolyl-propylamine C-terminal group were explored to further improve the activity. This is the first example of inhibitors of SH2 domains with sub-nanomolar affinity reported to date.