GlyH 101

Based on 171 reference(s) in Google Scholar 10 10 171

Axon 2572

CAS [328541-79-3]

MF C19H15Br2N3O3
MW 493.15

Purity: 98%
Soluble in DMSO

GlyH 101

Description

Highly potent and selective cystic fibrosis (CF) transmembrane regulator (CFTR) inhibitor (Ki value 4.3 µM in CFTR-expressing FRT cells) targeting mitochondrial functions, independently of chloride channel inhibition. GlyH 101 induces a rapid increase in ROS levels and depolarizes mitochondria in the four cell types, suggesting that these effects are independent of CFTR inhibition. Moreover, intraluminal GlyH 101 (2.5 g) reduced by 80% cholera toxin-induced intestinal fluid secretion in a closed-loop model of cholera.

C. Muanprasat et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: mechanism, structure-activity analysis, and in vivo efficacy. J Gen Physiol. 2004 Aug;124(2):125-37.

M Kelly et al. Cystic fibrosis transmembrane regulator inhibitors CFTR(inh)-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J Pharmacol Exp Ther. 2010 Apr;333(1):60-9.

Apoptosis Cardiovascular Cell Signaling & Oncology CNS Diabetes & Metabolism Miscellaneous Pain & Inflammation CFTR NF-κB MAPK EC 3.6.3.49

Highly potent and selective CFTR inhibitor

Chemical name

N'-(3,5-dibromo-2,4-dihydroxybenzylidene)-2-(naphthalen-2-ylamino)acetohydrazide

Parent CAS No.

[328541-79-3]

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GlyH 101

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GlyH 101

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