574729-26-3

Upstream product

• 574729-25-2 tert-butyl 3-amino-5-nitro-1H-indazole-1-carboxylate 
• 17417-09-3 2-fluoro-5-nitrobenzonitrile 
• 24424-99-5 di-tert-butyl dicarbonate 
• 41339-17-7 5-nitro-1H-indazol-3-amine 

Downstream Products

• 942189-48-2 3-amino-5-[(1-{2-oxo-2-[4-(4-pyrimidin-2-yl-phenyl)-piperazin-1-yl]ethyl}-pyrrolidine-3-carbonyl)-amino]-indazole-1-carboxylic acid tert-butyl ester 
• 574729-27-4 3-Amino-5-[4-tert-butoxycarbonylamino-2-(3,4-dichloro-phenyl)-butyrylamino]-indazole-1-carboxylic acid tert-butyl ester 
• 871708-10-0 1-(3-amino-1H-indazol-5-yl)-3-(4-benzyloxy-phenyl)-urea hydrochloridre 
• 871708-00-8 N-(3-amino-1H-indazol-5-yl)-2-(3-hydroxy-phenyl)-acetamide hydrochloride 
• 1268262-12-9 C₂₅H₃₀ClN₅O₅ 
• 1268262-16-3 C₂₀H₂₁ClN₄O₃ 
• 1003604-68-9 tert-butyl-3-amino-5-{3-[2-(3-methoxyphenyl)ethyl]ureido}indazole-1-carboxylate 
• 1003604-62-3 tert-butyl-3-amino-5-[3-(3-methoxybenzyl)ureido]indazole-1-carboxylate 

Relevant academic research and scientific papers

Design of Small Molecules That Compete with Nucleotide Binding to an Engineered Oncogenic KRAS Allele

RAS mutations are found in 30% of all human cancers, with KRAS the most frequently mutated among the three RAS isoforms (KRAS, NRAS, and HRAS). However, directly targeting oncogenic KRAS with small molecules in the nucleotide-binding site has been difficult because of the high affinity of KRAS for GDP and GTP. We designed an engineered allele of KRAS and a covalent inhibitor that competes for GTP and GDP. This ligand-receptor combination demonstrates that the high affinity of GTP and GDP for RAS proteins can be overcome with a covalent inhibitor and a suitably engineered binding site. The covalent inhibitor irreversibly modifies the protein at the engineered nucleotide-binding site and is able to compete with GDP and GTP. This provides a new tool for studying KRAS function and suggests strategies for targeting the nucleotide-binding site of oncogenic RAS proteins.

In Silico HTS and Structure Based Optimization of Indazole-Derived ULK1 Inhibitors

We present the outcome of an in silico high throughput screen (HTS) and optimization of a small molecule Unc-51-Like Kinase 1 (ULK1) inhibitor hit, SR-17398, with an indazole core. Docking studies guided design efforts that led to inhibitors with increase

Protein kinase affinity reagents based on a 5-aminoindazole scaffold

Affinity reagents that target protein kinases are powerful tools for signal transduction research. Here, we describe a general set of kinase ligands based on a 5-aminoindazole scaffold. This scaffold can readily be derivatized with diverse binding elements and immobilized analogs allow selective enrichment of protein kinases from complex mixtures.

Indazole compounds useful as protein kinase inhibitors

The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein R1, R2, V1, V2, and V3 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of AKT, PKA, PDK1, p70S6K, or ROCK kinase, mammalian protein kinases involved in proliferative and neurodegenerative disorders. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of utilizing those compositions in the treatment of various disorders.