32046-86-9

Usage

Structure

Aromatic organic compound with a benzene ring fused to an imidazole ring

Characteristic groups

Nitro group and chlorine atom attached to the benzene ring

Usage

Intermediate in the synthesis of various pharmaceuticals and agrochemicals

Versatility

Building block for the preparation of other organic compounds

Precautions

Potential hazards to human health and the environment, handle with care.

Upstream product

• 95-83-0 4-Chloro-1,2-phenylenediamine 
• 1123-92-8 5-chloro-benzo[1,2,5]selenadiazole 
• 20718-46-1 5-chloro-4-nitro-2,1,3-benzoselenadiazole 
• 144729-44-2 4-chloro-3-nitro-1,2-phenylenediamine 
• 122-51-0 orthoformic acid triethyl ester 

Downstream Products

• 1422955-34-7 C₁₃H₈ClFN₄O₂ 

Relevant academic research and scientific papers

INHIBITION OF HIF-2α HETERODIMERIZATION WITH HIF1β (ARNT)

Provided is a method of inhibiting heterodimerization of HIF-2α to HIF1β (ARNT) comprising binding certain small molecules to the HIF-2α PAS-B domain cavity but not to HIF1α and inhibiting HIF-2α heterodimerization to HIF1β (ARNT) but not inhibiting HIF1α

Development of inhibitors of the PAS-B domain of the HIF-2α transcription factor

Hypoxia inducible factors (HIFs) are heterodimeric transcription factors induced in a variety of pathophysiological settings, including cancer. We describe the first detailed structure-activity relationship study of small molecules designed to inhibit HIF-2α-ARNT heterodimerization by binding an internal cavity of the HIF-2α PAS-B domain. Through a series of biophysical characterizations of inhibitor-protein interactions (NMR and X-ray crystallography), we have established the structural requirements for artificial inhibitors of the HIF-2α-ARNT PAS-B interaction. These results may serve as a foundation for discovering therapeutic agents that function by a novel mode of action.