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Kifunensine

Catalog No.
B7315
Inhibitor of class I α-mannosidases that inhibits glycoprotein processing
Grouped product items
SizePriceStock Qty
1mg
$110.00
Ship with 5-10 days
5mg
$494.00
Ship with 5-10 days
10mg
$713.00
Ship with 5-10 days
50mg
$2,190.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Kifunensine is a potent and selective inhibitor of class I α-mannosidases and may serve as a key inhibitor of glycoprotein biosynthesis[1]. Kifunensine inhibits both human endoplasmic reticulum α-1,2-mannosidase I and members of the Golgi subfamily of the class I mannosidases (Golgi α-mannosidase IA, IB, and IC) exhibiting Ki values of 130 and 23 nM, respectively. It also inhibits mung bean α-1,2-mannosidase I with an IC50 value of 20-50 nM[1]. Kifunensine can be used to block α-mannosidase I activity at the endoplasmic reticulum (ER), preventing the removal of desired mutated proteins through ER quality control mechanisms[2,3]. 

References:

[1]. Hering K W, Karaveg K, Moremen K W, et al. A Practical Synthesis of Kifunensine Analogues as Inhibitors of Endoplasmic Reticulum alpha-Mannosidase I. Journal of Organic Chemistry, 2005, 70(24): p.9892-9904.

[2]. Bartoli M, Gicquel E, Barrault L, et al. Mannosidase I inhibition rescues the human α-sarcoglycan R77C recurrent mutation. Human Molecular Genetics, 2008, 17(9): 1214-1221.

[3]. Soheili T, Gicquel E, Poupiot J, et al. Rescue of sarcoglycan mutations by inhibition of endoplasmic reticulum quality control is associated with minimal structural modifications. Human Mutation, 2012, 33(2): 429-439.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt232.19
Cas No.109944-15-2
FormulaC8H12N2O6
SolubilitySoluble in H2O
Chemical Name(5R,6R,7S,8R,8aS)-6,7,8-trihydroxy-5-(hydroxymethyl)hexahydroimidazo[1,2-a]pyridine-2,3-dione
SDFDownload SDF
Canonical SMILESVO[[email protected]@H]([[email protected]]1O)[[email protected]@H](NC2=O)N(C2=O)[[email protected]](CO)[[email protected]]1O
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Protocol

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

Quality Control & MSDS

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Chemical structure

Kifunensine