| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Class I α-mannosidases (ER α-1,2-mannosidase I and Golgi Class I mannosidases IA, IB, IC).
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|---|---|
| ln Vitro |
The actinomycete Kitasatosporia kifunense 9482 is the source of the alkaloid kifunensine. It can inhibit N-glycan synthesis at the an8GlcNAc2 (Man8) or Man9GlcNAc2 (Man9) stage and is the most potent α-mannosidase I inhibitor [3].
Kifunensine inhibits human endoplasmic reticulum α-1,2-mannosidase I and Golgi Class I mannosidases IA, IB, and IC with Ki values of 130 nM and 23 nM, respectively. It is the most efficient inhibitor of α-mannosidase I. Kifunensine (2 µg/mL) significantly reduces lentil lectin binding in hybridoma cells expressing a human IgG1 monoclonal antibody. It is the most effective among the inhibitors tested in producing antibodies containing oligomannose residues without fucose. Kifunensine disrupts normal trafficking of the GLUT1 transporter, leading to decreased glucose uptake in human renal epithelial cells. It impairs tumour cell aggregation in human ovarian cancer cells in vitro. |
| ln Vivo |
In vivo efficacy of kifunensine has not been extensively characterized in publicly available literature. As a glycoprotein processing inhibitor, it would be expected to affect protein glycosylation and trafficking in vivo. Specific animal model data and dosing regimens are limited in publicly available sources. The compound is primarily used as a tool in cell culture and biochemical studies.
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| Enzyme Assay |
Class I α-mannosidase inhibition is assessed using in vitro enzyme assays with purified α-mannosidase enzymes (ER α-1,2-mannosidase I, Golgi mannosidase IA, IB, IC) and a fluorogenic substrate (e.g., 4-methylumbelliferyl-α-D-mannopyranoside). The release of the fluorescent 4-methylumbelliferone is measured. Ki values are calculated from enzyme kinetics. Cellular assays are used to assess the effect of kifunensine on N-glycan processing.
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| Cell Assay |
RT-PCR[3]
Cell Types: hybridoma cells expressing human IgG1 monoclonal antibody [3]. Tested Concentrations: 2 micrograms/ml. Incubation Duration: 4 days. Experimental Results: Significant reduction in lentil lectin binding. Kifunensine was the most effective of the inhibitors tested in producing antibodies containing oligomannose residues but no fucose. Cellular activity is evaluated in various cell lines, including hybridoma cells, human renal epithelial cells, and ovarian cancer cells. Cells are treated with kifunensine at various concentrations (typically 0.1-10 µg/mL) for 1-7 days. N-glycan processing is assessed by lectin binding (e.g., lentil lectin) or by mass spectrometry analysis of N-glycans. GLUT1 trafficking is assessed by measuring glucose uptake using radiolabeled glucose or fluorescent glucose analogs. Cell aggregation is assessed in ovarian cancer cells. Antibody glycoform analysis is performed by mass spectrometry. |
| Animal Protocol |
Animal/Disease Models: BALB/c mouse[3].
Doses: 5 mg/kg. Route of Administration: intravenously (iv) (iv)(iv) via tail vein. Experimental Results: There were no significant differences in serum levels of anti-TEM B mAb produced by cells treated with or without kifunensine over a 7-day period. In vivo studies for kifunensine are limited. Potential studies could be conducted in mouse models to assess the effects of kifunensine on glycoprotein processing and function in vivo. The compound would be administered via various routes (intraperitoneal, intravenous). Glycoprotein glycosylation patterns would be analyzed in tissues and serum. Specific protocols are not detailed in publicly available literature. |
| ADME/Pharmacokinetics |
Kifunensine has a molecular formula of C8H12N2O6 and a molecular weight of 232.19 g/mol. CAS Number: 109944-15-2. Purity is typically ≥99%. The compound is soluble in DMSO (up to 35 mg/mL) and water (up to 5 mM). Storage: Powder at -20°C for 3 years; in solvent at -80°C for 2 years or at -20°C for 1 year. The compound is an alkaloid from actinomycete Kitasatosporia kifunense.
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| Toxicity/Toxicokinetics |
Safety data for kifunensine indicate it is a research compound for laboratory use only. It should be handled with standard laboratory safety precautions. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval. Standard laboratory safety practices should be followed, including the use of personal protective equipment and adequate ventilation. Toxicity: Standard Handling (A).
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| References |
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| Additional Infomation |
There have been reports of kifurine being present in Kitasatospora kifunensis, and relevant data are available for reference.
Kifunensine is a research tool compound for studying glycoprotein processing, N-glycosylation, and ERAD. It is not approved for clinical use. The compound is a potent and selective inhibitor of class I α-mannosidases, making it a valuable tool for glycobiology research. Kifunensine is used to produce glycoproteins with specific glycoforms (e.g., oligomannose-type N-glycans) for structural and functional studies. It is also used to study the role of N-glycosylation in protein folding, trafficking, and function. Kifunensine has been used to produce antibodies with enhanced antibody-dependent cellular cytotoxicity (ADCC) due to the absence of core fucosylation. |
| Molecular Formula |
C8H12N2O6
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|---|---|
| Molecular Weight |
232.19068
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| Exact Mass |
232.069
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| CAS # |
109944-15-2
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| PubChem CID |
130611
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| Appearance |
White to off-white solid powder
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| Density |
1.9±0.1 g/cm3
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| Melting Point |
>280℃
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| Index of Refraction |
1.706
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| LogP |
-2.21
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
16
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| Complexity |
335
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C([C@@H]1[C@H]([C@@H]([C@@H]([C@@H]2N1C(=O)C(=O)N2)O)O)O)O
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| InChi Key |
OIURYJWYVIAOCW-PQMKYFCFSA-N
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| InChi Code |
InChI=1S/C8H12N2O6/c11-1-2-3(12)4(13)5(14)6-9-7(15)8(16)10(2)6/h2-6,11-14H,1H2,(H,9,15)/t2-,3-,4+,5+,6+/m1/s1
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| Chemical Name |
(5R,6R,7S,8R,8aS)-6,7,8-trihydroxy-5-(hydroxymethyl)-1,5,6,7,8,8a-hexahydroimidazo[1,2-a]pyridine-2,3-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~11.9 mg/mL (~51.25 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.19 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.19 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.19 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3068 mL | 21.5341 mL | 43.0682 mL | |
| 5 mM | 0.8614 mL | 4.3068 mL | 8.6136 mL | |
| 10 mM | 0.4307 mL | 2.1534 mL | 4.3068 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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