Kifunensine
Kifunensine (CAS 109944-15-2) is a selective inhibitor of class I α-mannosidases, enzymes critical for glycoprotein processing and folding. It primarily inhibits human endoplasmic reticulum α-1,2-mannosidase I and Golgi α-mannosidases IA, IB, and IC with Ki values of approximately 130 nM and 23 nM, respectively. Additionally, it suppresses plant-derived α-1,2-mannosidase I at IC50 values between 20–50 nM. By blocking α-mannosidase I activity in the endoplasmic reticulum (ER), kifunensine prevents the ER-associated degradation of misfolded glycoproteins, thus serving as an investigative tool in studies of protein quality control pathways and glycoprotein biosynthesis.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 232.19 |
Cas No. | 109944-15-2 |
Formula | C8H12N2O6 |
Solubility | Soluble in H2O |
Chemical Name | (5R,6R,7S,8R,8aS)-6,7,8-trihydroxy-5-(hydroxymethyl)hexahydroimidazo[1,2-a]pyridine-2,3-dione |
SDF | Download SDF |
Canonical SMILES | VO[C@@H]([C@H]1O)[C@@H](NC2=O)N(C2=O)[C@H](CO)[C@H]1O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
Hybridoma cells expressing a human IgG1 monoclonal antibody against a tumor vascular associated antigen |
Reaction Conditions |
2 μg/mL kifunensine for 4 d incubation |
Applications |
Kifunensine treatment significantly reduced the lentil lectin binding. Furthermore, kifunensine was the most effective among the glycosylation inhibitors tested in producing antibodies containing oligomannose residues without fucose. |
Animal experiment:[1] | |
Animal models |
BALB/c mice |
Dosage form |
5 mg/kg Injected via the tail vein |
Applications |
The serum levels of antibody in mice were not significantly altered up to 168 h following injection. The use of kifunensine provided a simple and rapid method for the production of antibodies with increased antibody-dependent cell mediated cytotoxicity (ADCC) without the time-consuming need to re-engineer either the antibody molecule or the host cell line. |
Note |
The technical data provided above is for reference only. |
References: 1. Zhou Q, Shankara S, Roy A, et al. Development of a simple and rapid method for producing non-fucosylated oligomannose containing antibodies with increased effector function. Biotechnology and Bioengineering, 2008, 99(3): 652-665. |
Quality Control & MSDS
- View current batch:
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
