Bioactivity | Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-FU (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation[1][2][3]. | ||||||||||||
Target | O-glycosylation. | ||||||||||||
Invitro | Benzyl-α-GalNAc (5 mM; 72 h) inhibits O-glycosylation of mucin in SUIT-2 cells[1].Benzyl-α-GalNAc (2, 4 mM; 48 h) inhibits the proliferation and activation of LX-2 cells[2].Benzyl-α-GalNAc (2, 4 mM; 48 h) decreases collagen expression in LX-2 cells[2]. Cell Viability Assay[1] Cell Line: | ||||||||||||
In Vivo | Benzyl-α-GalNAc (1 mg/mice; tumoural injection; single daily; days 4, 6, 8 and 10 after tumour size reaches 50-70 mm3) enhances the anti-tumour activity of 5-FU by inhibiting O-glycosylation in mice[3].(Mucin overexpression limits the effectiveness of 5-FU by reducing intracellular drug uptake and antineoplastic drug effects in pancreatic tumours) Animal Model: | ||||||||||||
Name | Benzyl-α-GalNAc | ||||||||||||
CAS | 3554-93-6 | ||||||||||||
Formula | C15H21NO6 | ||||||||||||
Molar Mass | 311.33 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Kalra AV, et al. Mucin impedes cytotoxic effect of 5-FU against growth of human pancreatic cancer cells: overcoming cellular barriers for therapeutic gain. Br J Cancer. 2007 Oct 8;97(7):910-8. Epub 2007 Oct 2. [2]. Kalra AV, et al. Mucin overexpression limits the effectiveness of 5-FU by reducing intracellular drug uptake and antineoplastic drug effects in pancreatic tumours. Eur J Cancer. 2009 Jan;45(1):164-73. [3]. Fan X, et al. Protein O glycosylation regulates activation of hepatic stellate cells. Inflammation. 2013 Dec;36(6):1248-52. https://pubmed.ncbi.nlm.nih.gov/23743764/ |