GlyH-101

• CAT Number: I013891
• CAS Number: 328541-79-3
• Molecular Formula: C19H15Br2N3O3
• Molecular Weight: 493.15
• Purity: ≥95%
• Synonyms: N-[(E)-(3,5-dibromo-2,4-dihydroxyphenyl)methylideneamino]-2-(naphthalen-2-ylamino)acetamide
• InChI: InChI=1S/C19H15Br2N3O3/c20-15-8-13(18(26)17(21)19(15)27)9-23-24-16(25)10-22-14-6-5-11-3-1-2-4-12(11)7-14/h1-9,22,26-27H,10H2,(H,24,25)/b23-9+
• InChIKey: RMBDLOATEPYBSI-NUGSKGIGSA-N
• SMILES: C1=CC=C2C=C(C=CC2=C1)NCC(=O)NN=CC3=CC(=C(C(=C3O)Br)O)Br

GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current[1][2].
GlyH-101 (0-50 µM) shows antiproliferative activity in PCT and PS120 cells[1].
GlyH-101 (0.5, 1, 5, 10 µM) inhibits CFTR-like current in a concentration-dependent manner in PCT cells[1].
GlyH-101 (0.5, 1, 5, 10 µM) inhibits the VSORC current with IC50s of 5.38, 6.26 µM for PS120, PCT cells, respectively[1].
GlyH-101 (2.5 µg) reduces by about 80% cholera toxin-induced intestinal fluid secretion in mouse[2].

Reference

[1]. Muanprasat C, 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.
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[2]. Kelly M, 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.
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[3]. Barman PP, et al. Cardiac ion channel current modulation by the CFTR inhibitor GlyH-101. Biochem Biophys Res Commun. 2011 Apr 29;408(1):12-7.
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[4]. Melis N, et al. Revisiting CFTR inhibition: a comparative study of CFTRinh -172 and GlyH-101 inhibitors. Br J Pharmacol. 2014 Aug;171(15):3716-27.
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[5]. Muanprasat C, 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.
 [Content Brief]