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几夫碱

几夫碱用途

Kifunensine 是可从放线菌中分离得到的 I 类 α-mannosidases 有效选择性抑制剂,可阻断 α-mannosidases I 修剪糖蛋白上的甘露糖残基。Kifunensine 可抑制内质网相关蛋白降解途径。

几夫碱名称

[ CAS 号 ]:
109944-15-2

[ 中文名 ]:
几夫碱

[ 英文名 ]:
Kifunensine

[英文别名 ]:

KIFUNENSINE,KITASATOSPORIA KIFUNENSE
1-deoxymannojirimycin
Kifunensine

几夫碱生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[体外研究]

Kifunensine是一种来自放线菌kifunense 9482的生物碱,是a-甘露糖苷酶I最有效的抑制剂,在an8GlcNAc2(Man8)或Man9GlcNAc2(Man9)阶段阻断N-聚糖的合成[3]。RT-PCR[3]。细胞系：表达人IgG1单克隆抗体的杂交瘤细胞[3]。浓度：2μg/mL,培养时间：4天。结果：扁豆凝集素结合明显降低。在所测试的抑制剂中,Kifunensine是最有效的产生抗体的低聚甘露糖残基不含岩藻糖。

[体内研究]

动物模型：BALB/c小鼠[3]。剂量：5mg/kg。给药：尾静脉注射。结果：用或不加kifunensine处理细胞产生的抗temb单克隆抗体在7d内无明显差异。

[参考文献]

[1]. Yongao Xiong, et al. Glycoform Modification of Secreted Recombinant Glycoproteins through Kifunensine Addition during Transient Vacuum Agroinfiltration. Int J Mol Sci. 2018 Mar; 19(3): 890.

[2]. Hiroshi Kayakiri, et al. Structure of Kifunensine, a New Immunomodulator Isolated from an Actinomycete. J. Org. Chem. 1989,54,4015-4016.

[3]. Qun Zhou, et al. Development of a Simple and Rapid Method for Producing Non-Fucosylated Oligomannose Containing Antibodies With Increased Effector Function. Biotechnol Bioeng. 2008 Feb 15;99(3):652-65.

[4]. Hyung Lim Elfrink, et al. Inhibition of Endoplasmic Reticulum Associated Degradation Reduces Endoplasmic Reticulum Stress and Alters Lysosomal Morphology and Distribution. Mol Cells. 2013 Apr 30; 35(4): 291–297.

几夫碱物理化学性质

[ 密度 ]:
1.9±0.1 g/cm3

[ 熔点 ]:
>280â„ƒ

[ 分子式 ]:
C₈H₁₂N₂O₆

[ 分子量 ]:
232.191

[ 精确质量 ]:
232.069534

[ PSA ]:
130.33000

[ LogP ]:
-2.21

[ 折射率 ]:
1.706

[ 储存条件 ]:
-20°C

几夫碱MSDS

详细MSDS(安全技术说明书)

几夫碱安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
NONH for all modes of transport

几夫碱合成路线

详细合成路线

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几夫碱文献

A context-independent N-glycan signal targets the misfolded extracellular domain of Arabidopsis STRUBBELIG to endoplasmic-reticulum-associated degradation.

Biochem. J. 464(3) , 401-11, (2014)

N-glycosylation of proteins plays an important role in the determination of the fate of newly synthesized glycoproteins in the endoplasmic reticulum (ER). Specific oligosaccharide structures recruit m...

Synthesis of kifunensine thioanalogs and their inhibitory activities against HIV-RT and α-mannosidase.

Carbohydr. Res. 365 , 1-8, (2013)

An efficient and practical synthesis of kifunensine thioanalogs 1a-c was reported. The bicyclic azasugars fused thiazolidin-4-one 4a-c as key intermediates were first synthesized in good yields of 74-...

Evolution of cross-neutralizing antibody specificities to the CD4-BS and the carbohydrate cloak of the HIV Env in an HIV-1-infected subject.

PLoS ONE 7(11) , e49610, (2012)

Broadly neutralizing antibodies are considered an important part of a successful HIV vaccine. A better understanding of the factors underlying their development during infection and of the epitopes th...

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几夫碱