1200126-26-6

Basic information

• Product Name: GNE 900
• Synonyms: GNE 900;PPYHOOZGDDPLKM-UHFFFAOYSA-N
• CAS NO: 1200126-26-6
• Molecular Formula: C₂₃H₂₁N₅
• Molecular Weight: 367.44634
• Mol File: 1200126-26-6.mol
• Article Data: 2

Chemical Properties

• Appearance: /
• CAS DataBase Reference: GNE 900(CAS DataBase Reference)
• NIST Chemistry Reference: GNE 900(1200126-26-6)
• EPA Substance Registry System: GNE 900(1200126-26-6)

Safety Data

• Hazardous Substances Data: 1200126-26-6(Hazardous Substances Data)

Usage

General Description

GNE 900 is a potent and selective inhibitor of the selective inhibitor of inositol trisphosphate 3-kinase (IP3K), which plays a key role in regulating calcium signaling in cells. By inhibiting IP3K, GNE 900 disrupts the signaling pathway that controls calcium release from intracellular stores, ultimately leading to a decrease in cellular calcium levels. This inhibition has been shown to have potential therapeutic applications in the treatment of various diseases, including cancer, neurodegenerative disorders, and autoimmune diseases. GNE 900 has demonstrated promising results in preclinical studies, and its development as a potential drug candidate is ongoing.

Upstream product

• 1200130-52-4 3-bromo-9H-pyrrolo[2,3-b:5,4-c′]dipyridine-6-carbonitrile 
• 1200434-84-9 (4-(piperidin-1-ylmethyl)phenyl)boronic acid 
• 1200130-50-2 methyl 3-bromo-9H-pyrrolo[2,3-b:5,4-c′]dipyridine-6-carboxylate 
• 1200130-51-3 3-bromo-9H-pyrrolo[2,3-b:5,4-c′]dipyridine-6-carboxamide 

Relevant articles and documents

Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1

Checkpoint kinase 1 (ChK1) plays a key role in the DNA damage response, facilitating cell-cycle arrest to provide sufficient time for lesion repair. This leads to the hypothesis that inhibition of ChK1 might enhance the effectiveness of DNA-damaging therapies in the treatment of cancer. Lead compound 1 (GNE-783), the prototype of the 1,7-diazacarbazole class of ChK1 inhibitors, was found to be a highly potent inhibitor of acetylcholine esterase (AChE) and unsuitable for development. A campaign of analogue synthesis established SAR delineating ChK1 and AChE activities and allowing identification of new leads with improved profiles. In silico docking using a model of AChE permitted rationalization of the observed SAR. Compounds 19 (GNE-900) and 30 (GNE-145) were identified as selective, orally bioavailable ChK1 inhibitors offering excellent in vitro potency with significantly reduced AChE activity. In combination with gemcitabine, these compounds demonstrate an in vivo pharmacodynamic effect and are efficacious in a mouse p53 mutant xenograft model.