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-Fluorouracil (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation.

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CAS No. : 3554-93-6

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Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Benzyl-α-GalNAc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 8:e2415941.  [Abstract]

    Benzyl-α‐GalNAc (BAGN; 25 mg/kg; i.v.). Western blot analysis of O‐GlcNAc, LIMA1, OGT, OGA, α‐SMA, and Col3A1 in livers from NCD‐fed mice, HFD‐fed mice, and HFD‐fed mice injected with BAGN.

    Benzyl-α-GalNAc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 8:e2415941.  [Abstract]

    Benzyl-α‐GalNAc (BAGN; 25 mg/kg; i.v.). Immunofluorescence showing LIMA1 (red) and O‐GlcNAc (green) colocalization in livers from NCD‐fed mice, HFD‐fed mice, and HFD‐fed mice injected with BAGN.

    Benzyl-α-GalNAc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 8:e2415941.  [Abstract]

    Benzyl-α-GalNAc (BAGN; 25 mg/kg; i.v.). Changes in body weight of NCD‐fed mice, HFD‐fed mice, and HFD‐fed mice injected with BAGN.

    Benzyl-α-GalNAc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 8:e2415941.  [Abstract]

    Benzyl-α-GalNAc (BAGN; 25 mg/kg; i.v.). Tunel and Oil red O staining in livers from NCD‐fed mice, HFD‐fed mice, and HFD‐fed mice injected with BAGN.

    Benzyl-α-GalNAc purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 8:e2415941.  [Abstract]

    Benzyl-α-GalNAc (BAGN; 25 mg/kg; i.v.). Lipometabolic mRNA expression in the liver of NCD‐fed mice, HFD‐fed mice, and HFD‐fed mice injected with BAGN.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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-Fluorouracil (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.

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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.93%

    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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    Product Name:
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