Concanamycin A (Synonyms: Antibiotic X 4357B； NSC 674620； X 4357B) |
Catalog No.GC17519
One-Click Copy Product Info
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Concanamycin A, a macrolide antibiotic, is a specific inhibitor of vacuolar-type ATPase (V-ATPase) with an IC50 value of 10nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 80890-47-7
Sample solution is provided at 25 µL, 10mM.
Concanamycin A, a macrolide antibiotic, is a specific inhibitor of vacuolar-type ATPase (V-ATPase) with an IC50 value of 10nM[1]. Concanamycin A counteracts the HIV accessory protein Nef, reversing the MHC-I downregulation mediated by Nef, thereby enhancing the clearance of HIV-infected primary lymphocytes by cytotoxic T lymphocytes (CTL)[2]. Concanamycin A has been widely used to block growth of Neurospora crassa in medium adjusted to pH 7[3].
In vitro, Concanamycin A (12nM) pretreatment for 4 hours significantly inhibited the production of nitric oxide in mouse peritoneal macrophages induced by Lipopolysaccharide (LPS) (1µg/ml), reduced the expression of TLR4 molecules on the cell surface, and decreased the activation of NF-κB[4]. Treatment with 2nM Concanamycin A for 48 hours triggered apoptosis in human submandibular gland ductal carcinoma cells, accompanied by nuclear condensation, DNA fragmentation, and a decrease in the level of heat shock protein 27 (HSP27)[5]. Treatment with 10nM Concanamycin A for 24 hours restrained the growth of RAW 264.7 cells and disrupted the mitochondrial membrane potential[6]. 3nM Concanamycin A treatment for 24 hours upregulated the tyrosinase activity in FM3 and B16-G4F cells, promoting melanin production[7].
References:
[1] Huss M, Ingenhorst G, König S, et al. Concanamycin A, the specific inhibitor of V-ATPases, binds to the Vo subunit c[J]. Journal of Biological Chemistry, 2002, 277(43): 40544-40548.
[2] Painter M M, Zimmerman G E, Merlino M S, et al. Concanamycin A counteracts HIV-1 Nef to enhance immune clearance of infected primary cells by cytotoxic T lymphocytes[J]. Proceedings of the National Academy of Sciences, 2020, 117(38): 23835-23846.
[3] Bowman E J, O'Neill F J, Bowman B J. Mutations of pma-1, the gene encoding the plasma membrane H+-ATPase of Neurospora crassa, suppress inhibition of growth by concanamycin A, a specific inhibitor of vacuolar ATPases[J]. Journal of biological chemistry, 1997, 272(23): 14776-14786.
[4] Eswarappa S M, Basu N, Joy O, et al. Folimycin (concanamycin A) inhibits LPS-induced nitric oxide production and reduces surface localization of TLR4 in murine macrophages[J]. Innate Immunity, 2008, 14(1): 13-24.
[5] Aiko K, Tsujisawa T, Koseki T, et al. Involvement of cytochrome c and caspases in apoptotic cell death of human submandibular gland ductal cells induced by concanamycin A[J]. Cellular signalling, 2002, 14(8): 717-722.
[6] Hong J J, Nakano Y, Yokomakura A, et al. Nitric oxide production by the vacuolar-type (H+)-ATPase inhibitors bafilomycin A1 and concanamycin A and its possible role in apoptosis in RAW 264.7 cells[J]. The Journal of pharmacology and experimental therapeutics, 2006, 319(2): 672-681.
[7] Ancans J, Thody A J. Activation of melanogenesis by vacuolar type H+-ATPase inhibitors in amelanotic, tyrosinase positive human and mouse melanoma cells[J]. FEBS letters, 2000, 478(1-2): 57-60.
| Cell experiment [1]: | |
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Cell lines |
Peritoneal macrophages from C57/BL6 mice |
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Preparation Method |
Peritoneal macrophages were cultured in RPMI-1640 medium, supplemented 10% heat-inactivated fetal bovine serum at 37°C in an incubator with 5% CO2. Cells were seeded in a 6-well plate at a density of 3×105 cells/well overnight. Cells were treated with different concentrations of Concanamycin A (0, 3, 6, 9, and 12nM) for 4h. After 4h, 1µg/ml of LPS was added and incubated for 12h. The LPS-induced nitric oxide production was measured. |
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Reaction Conditions |
0, 3, 6, 9, and 12nM; 4h |
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Applications |
Concanamycin A treatment reduced LPS-induced nitric oxide production within peritoneal macrophages in a dose-dependent manner. |
References: [1] Eswarappa S M, Basu N, Joy O, et al. Folimycin (concanamycin A) inhibits LPS-induced nitric oxide production and reduces surface localization of TLR4 in murine macrophages[J]. Innate Immunity, 2008, 14(1): 13-24. | |
| Cas No. | 80890-47-7 | SDF | |
| Synonyms | Antibiotic X 4357B； NSC 674620； X 4357B | ||
| Chemical Name | (3Z,5E,7R,8R,9S,10S,11R,13E,15E,17S,18R)-18-[(1S,2R,3S)-3-[(2R,4R,5S,6R)-4-[[4-O-(aminocarbonyl)-2,6-dideoxy-β-D-arabino-hexopyranosyl]oxy]tetrahydro-2-hydroxy-5-methyl-6-(1E)-1-propen-1-yl-2H-pyran-2-yl]-2-hydroxy-1-methylbutyl]-9-ethyl-8,10-dihydroxy-3, | ||
| Canonical SMILES | CCC1C(C(CC(=CC=CC(C(OC(=O)C(=CC(=CC(C1O)C)C)OC)C(C)C(C(C)C2(CC(C(C(O2)C=CC)C)OC3CC(C(C(O3)C)OC(=O)N)O)O)O)OC)C)C)O | ||
| Formula | C46H75NO14 | M.Wt | 866.09 |
| Solubility | Methanol : Soluble; DMSO : Soluble; Acetonitrile: Soluble | Storage | Store at -20°C, protect from light, Avoid solvent evaporation. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1546 mL | 5.7731 mL | 11.5461 mL |
| 5 mM | 230.9 μL | 1.1546 mL | 2.3092 mL |
| 10 mM | 115.5 μL | 577.3 μL | 1.1546 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00% Appearance: A solution in acetonitrile
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
JAM1 is degraded by the autophagy pathway and negatively regulates RKN resistance. c, d Response of WT and atg7 mutant seedlings to the ubiquitin proteasome inhibitor MG132, the vacuolar-type ATPase inhibitor ConcanamycinA (ConA) and the autophagy inducer AZD8055 with or without RKN infection.
Plants were soaked in 0.5X Linsmaier and Skoog (LS) liquid medium containing DMSO, 50 μM MG132, 5 μM AZD8055 or 1 μM ConA (Glpbio, GC17519).
Nat Commun 14.1 (2023): 4769. PMID: 37553319 IF: 16.6009 -
Related Biological Data
ZmNBR1 is not phosphorylated by ZmBRI1a, and ZmNBR1 promotes the autophagic degradation of ZmBRI1a (F) Immunoblot analysis of the ZmBRI1a protein levels. Plants were grown to the three‐leaf stage and treated with 20% PEG6000 (dehydration stress) with or without concanamycin A (Conc A) (1 μmol/L) for 12 h.
For autophagy inhibitor treatment, dimethyl sulfoxide, spautin‐1, or Conc A (1 μmol/L; GLPBIO, Montclair, CA, USA) was added to the PEG6000 treatment for 12 h.
J Integr Plant Biol (2024). PMID: 38607264 IF: 11.3997
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)