1. Epigenetics
  2. Glycosyltransferase
  3. Benzyl-α-GalNAc

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.

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Benzyl-α-GalNAc Chemical Structure

Benzyl-α-GalNAc Chemical Structure

CAS No. : 3554-93-6

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Customer Review

Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

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].

IC50 & Target

O-glycosylation[1][2][3].

In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SUIT-2 cells
Concentration: 5 mM
Incubation Time: 72 h
Result: Inhibited mucin O-glycosylation.

Cell Viability Assay[2]

Cell Line: LX-2 cells
Concentration: 2, 4 mM
Incubation Time: 48 h
Result: Remarkably decreased the expression of α-SMA in a dose-dependent manner (α-SMA is the marker for the activation of HSCs, which means that quiescent cells transform into myofibroblasts).

Cell Proliferation Assay[2]

Cell Line: LX-2 cells (PDGF-BB-induced)
Concentration: 2, 4 mM
Incubation Time: 48 h
Result: Partly reversed PDGF-BB-induced proliferation in cells.

Western Blot Analysis[2]

Cell Line: LX-2 cells
Concentration: 2, 4 mM
Incubation Time: 48 h
Result: Downregulated the mRNA levels of collagens I and III in a dose-dependent manner.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female severe combined immunodeficient (SCID) mice (6 to 8-week-old; capan-1 tumour model)[3].
Dosage: 1 mg/mice (in combination with 5-FU)
Administration: Tumoural injection; single daily; days 4, 6, 8 and 10 after tumour size reaches 50-70 mm3
Result: Significantly lowered neoplastic cells compared to 5-FU alone.
Molecular Weight

311.33

Formula

C15H21NO6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]([C@H]([C@@H](CO)O1)O)[C@@H](NC(C)=O)[C@H]1OCC2=CC=CC=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (321.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 7 mg/mL (22.48 mM; ultrasonic and warming and heat to 60°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2120 mL 16.0601 mL 32.1203 mL
5 mM 0.6424 mL 3.2120 mL 6.4241 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.95%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 3.2120 mL 16.0601 mL 32.1203 mL 80.3006 mL
5 mM 0.6424 mL 3.2120 mL 6.4241 mL 16.0601 mL
10 mM 0.3212 mL 1.6060 mL 3.2120 mL 8.0301 mL
15 mM 0.2141 mL 1.0707 mL 2.1414 mL 5.3534 mL
20 mM 0.1606 mL 0.8030 mL 1.6060 mL 4.0150 mL
DMSO 25 mM 0.1285 mL 0.6424 mL 1.2848 mL 3.2120 mL
30 mM 0.1071 mL 0.5353 mL 1.0707 mL 2.6767 mL
40 mM 0.0803 mL 0.4015 mL 0.8030 mL 2.0075 mL
50 mM 0.0642 mL 0.3212 mL 0.6424 mL 1.6060 mL
60 mM 0.0535 mL 0.2677 mL 0.5353 mL 1.3383 mL
80 mM 0.0402 mL 0.2008 mL 0.4015 mL 1.0038 mL
100 mM 0.0321 mL 0.1606 mL 0.3212 mL 0.8030 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Benzyl-α-GalNAc
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