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Kifunensine

 
Catalog No.
B7315
I类α-甘露糖苷酶抑制剂,抑制糖蛋白加工
组合的产品项目
规格价格库存 数量
1mg
¥ 1,570.00
Ship with 10-15 days
5mg
¥ 5,308.00
Ship with 10-15 days
10mg
¥ 8,829.00
Ship with 10-15 days
50mg
¥ 20,529.00
Ship with 10-15 days

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背景

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.

化学属性

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[C@@H]([C@H]1O)[C@@H](NC2=O)N(C2=O)[C@H](CO)[C@H]1O
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一般建议不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

试验操作

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.

质量控制

质量控制和MSDS

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化学结构

Kifunensine