Echinomycin (Synonyms: Antibiotic A 654I； NSC 13502； NSC 526417； Quinomycin A； SK 302B) |
| Catalog No.GC18236 |
An inhibitor of HIF1mediated gene transcription
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 512-64-1
Sample solution is provided at 25 µL, 10mM.
Hypoxia-inducible factor-1 (HIF-1) is a transcription factor that controls genes involved in glycolysis, angiogenesis, migration, and invasion. Echinomycin is a cell-permeable inhibitor of HIF-1-mediated gene transcription.[1][2] It acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the hypoxia-responsive element.[1][2][3] Echinomycin reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50 value of 1.2 nM. It inhibits hypoxia-induced expression of vascular endothelial growth factor, blocking angiogenesis and altering excitatory synaptic transmission in hippocampal neurons.[2][4] Echinomycin also impairs expression of survivin, enhancing the sensitivity of multiple myeloma cells to melphalan.[5]
Reference:
[1]. Kong, D., Park, E.J., Stephen, A.G., et al. Echinomycin, a small-molecule inhibitor of hypoxia-inducible factor-1 DNA-binding activity Cancer Research 65(19), 9047-9055 (2005).
[2]. Nickols, N.G., Jacobs, C.S., Farkas, M.E., et al. Modulating hypoxia-inducible transcription by disrupting the HIF-1-DNA interface ACS Chemical Biology 2(8), 561-571 (2007).
[3]. Ward, D.C., Reich, E., and Goldberg, I.H. Base specificity in the interaction of polynucleotides with antibiotic drugs Science 149(3689), 1259-1263 (1965).
[4]. Huang, Y.F., Yang, C.H., Huang, C.C., et al. Pharmacological and genetic accumulation of hypoxia-inducible factor-1α enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor J. Neurosci. 30(17), 6080-6093 (2010).
[5]. Hu, Y., Kirito, K., Yoshida, K., et al. Inhibition of hypoxia-inducible factor-1 function enhances the sensitivity of multiple myeloma cells to melphalan Mol. Cancer Ther. 8(8), 2329-2338 (2009).
| Cas No. | 512-64-1 | SDF | |
| Synonyms | Antibiotic A 654I； NSC 13502； NSC 526417； Quinomycin A； SK 302B | ||
| Chemical Name | N-(2-quinoxalinylcarbonyl)-O-[N-(2-quinoxalinylcarbonyl)-D-seryl-L-alanyl-3-mercapto-N,S-dimethylcysteinyl-N-methyl-L-valyl]-D-seryl-L-alanyl-N-methylcysteinyl-N-methyl-(8→1)-lactone, cyclic (3→7)-thioether-L-valine | ||
| Canonical SMILES | O=C(NC(COC(C(C(C)C)N(C)C(C1CS2)=O)=O)C(NC(C)C(N(C(C2SC)C(N(C)C(C(OCC(NC(C3=NC(C=CC=C4)=C4N=C3)=O)C(NC(C(N1C)=O)C)=O)=O)C(C)C)=O)C)=O)=O)C5=NC6=C(N=C5)C=CC=C6 | ||
| Formula | C51H64N12O12S2 | M.Wt | 1101.3 |
| Solubility | Soluble in DMSO, Soluble in Methanol | Storage | Store at -20°C |
| 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. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.908 mL | 4.5401 mL | 9.0802 mL |
| 5 mM | 0.1816 mL | 0.908 mL | 1.816 mL |
| 10 mM | 0.0908 mL | 0.454 mL | 0.908 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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