Concanamycin A (Synonyms: Antibiotic X 4357B; NSC 674620; X 4357B) |
Katalog-Nr.GC17519 |
V-Typ (vakuolärer) H+-ATPase-Inhibitor
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.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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). |
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.
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. |
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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 | |||
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 ddH2O, 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.
Average Rating: 5
(Based on Reviews and 4 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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