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Concanamycin A (Synonyms: Antibiotic X 4357B; NSC 674620; X 4357B)

Katalog-Nr.GC17519

V-Typ (vakuolärer) H+-ATPase-Inhibitor

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Concanamycin A Chemische Struktur

Cas No.: 80890-47-7

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1,2]:

Cell lines

HCT-116, DLD-1, Colo206F, HeLa cells, Androgen-dependent (LNCaP) and androgen-independent (C4-2B) cells.

Preparation method

This compound is limited soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

20 nM, 60 min

Applications

CCA effectively attenuated the TRAIL-induced activation of caspases in TRAIL-sensitive colorectal cancer cell lines. In CCA-treated Colo206F cells, the number of M30-positive apoptotic cells gradually increased and almost reached the proportion seen in untreated cells within 3–4h after the addition of TRAIL. Treatment with CCA resulted in a lack of apoptosis-related chromatin condensation in DLD-1 cells incubated with TRAIL for 90 min. Treatment with nanomolar concentrations of concanamycin A reduced the in vitro invasion in LNCaP and C4-2B cell types by 80%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Horova V, et al., Inhibition of vacuolar ATPase attenuates the TRAIL-induced activation of caspase-8 and modulates the trafficking of TRAIL receptosomes. FEBS J, 2013. 280(14).

[2]. Michel V, et al., Inhibitors of vacuolar ATPase proton pumps inhibit human prostate cancer cell invasion and prostate-specific antigen expression and secretion. Int J Cancer. 2013.132(2).

Background

Concanamycin A ist ein spezifischer Inhibitor der Vakuolentyp-ATPase (V-ATPase) mit einem IC50-Wert von 10 nM [1].

Die Vakuolentyp-ATPase (V-ATPase) wird von klaren Zellen exprimiert, um das Lumen des Nebenhodens zu versauern, was für die männliche Fruchtbarkeit unerlässlich ist. Darüber hinaus führt sie zur Protonenausscheidung in das extrazelluläre Medium, was dazu beiträgt, den intrazellulären pH-Wert unter einem sauren Mikroumgebung aufrechtzuerhalten. Es wurde auch berichtet, dass V-ATPase an der Versauerung der Mikroumgebung rund um/in soliden Tumoren beteiligt ist und bei mehreren bösartigen Tumoren eine Tumorinvasion/Multidrugresistenz induziert [2].

Concanamycin A (CMA) ist ein spezifischer V-ATPase-Inhibitor und unterscheidet sich vom berichteten V-ATPase-Inhibitor SS33410. Bei oralen Plattenepithelkarzinomen (OSCC) führte die Behandlung von OSCC-Zelllinien (MISK81-5, SAS und HSC-4) mit niedriger Konzentration von CMA zur Apoptose der Tumorzellen [3]. Vorbehandelte Kolorektalkrebszelllinien mit Concanamycin A konnten durch Blockierung der endosomalen Azidifizierung durch V-ATPase signifikant die TRAIL-induzierte Apoptose des Tumor-Nekrose-Faktors (TNF)-verwandten Apoptose-induzierenden Liganden verbessern [4]. Bei einem Prostatakrebszellinie C4-2B reduzierte die Hemmung von V-ATPase durch Concanamycin A 80% Invasion in vitro [5].

Concanamycin A wurde auch als potenter Inhibitor der CTL-Zytotoxizität über den perforinvermittelten Zytotoxizitätsweg berichtet [6].

References:
[1].  Huss, M., et al., Concanamycin A, the specific inhibitor of V-ATPases, binds to the V(o) subunit c. J Biol Chem, 2002. 277(43): p. 40544-8.
[2].  Muroi, M., et al., Folimycin (concanamycin A), a specific inhibitor of V-ATPase, blocks intracellular translocation of the glycoprotein of vesicular stomatitis virus before arrival to the Golgi apparatus. Cell Struct Funct, 1993. 18(3): p. 139-49.
[3].  Kiyoshima, T., et al., Chemoresistance to concanamycin A1 in human oral squamous cell carcinoma is attenuated by an HDAC inhibitor partly via suppression of Bcl-2 expression. PLoS One, 2013. 8(11).
[4].  Horova V, et al., Inhibition of vacuolar ATPase attenuates the TRAIL-induced activation of caspase-8 and modulates the trafficking of TRAIL receptosomes. FEBS J, 2013. 280(14).
[5].  Michel V, et al., Inhibitors of vacuolar ATPase proton pumps inhibit human prostate cancer cell invasion and prostate-specific antigen expression and secretion. Int J Cancer. 2013.132(2).
[6].  Benkhoucha M et al., The neurotrophic hepatocyte growth factor attenuates CD8+ cytotoxic T-lymphocyte activity. J Neuroinflammation. 2013, 10.

Chemical Properties

Cas No. 80890-47-7 SDF
Überlieferungen 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
Löslichkeit Soluble in Acetonitrile; Soluble in DMSO; Soluble in Methanol Storage Store at -20°C, protect from light
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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.1546 mL 5.7731 mL 11.5461 mL
5 mM 0.2309 mL 1.1546 mL 2.3092 mL
10 mM 0.1155 mL 0.5773 mL 1.1546 mL
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