| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Threonyl-tRNA synthetase (ThrRS).
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|---|---|
| ln Vitro |
Borrelidin targets ALL cell lines and promotes apoptosis and mediates G1 arrest [1].
In vitro, borrelidin selectively inhibits threonyl-tRNA synthetase, an enzyme crucial for protein synthesis, in both bacterial and eukaryotic systems. It exhibits potent anti-angiogenic activity with an IC₅0 of 0.8 nM, disrupting capillary tubes and inhibiting their formation in rat aorta assays. The compound induces apoptosis in capillary tube-forming cells. Anti-angiogenesis effects are mediated through distinct pathways: threonyl-tRNA synthetase inhibition and caspase activation are independently involved in suppression of proliferation and induction of apoptosis in endothelial cells. |
| ln Vivo |
In vivo, borrelidin exhibits anti-angiogenic activity in a mouse model of tumor angiogenesis. It has been studied for its anti-viral, anti-bacterial, anti-malarial, and anti-angiogenic properties. The compound's potent anti-angiogenic activity makes it a compound of interest for cancer research.
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| Enzyme Assay |
ThrRS enzyme assays are performed using purified threonyl-tRNA synthetase from bacterial (e.g., E. coli) or eukaryotic sources. The assay mixture contains 50 mM Tris-HCl (pH 7.5), 20 mM MgCl2, 50 mM KCl, 2 mM ATP, 2 mM DTT, 10 microM [3H]-threonine, and tRNA. Borrelidin is added at concentrations ranging from 0.1 nM-10 microM. The reaction is initiated by adding enzyme, incubated at 37degC for 10-30 minutes, and terminated by trichloroacetic acid precipitation. Radioactivity incorporated into tRNA is measured by scintillation counting. IC₅0 values are calculated from dose-response curves. Anti-angiogenic activity is assessed using rat aortic ring assays: aortic rings are embedded in collagen or Matrigel and cultured with VEGF and borrelidin.
|
| Cell Assay |
Endothelial cells (e.g., HUVEC, human umbilical vein endothelial cells) are cultured in appropriate medium. Cells are seeded in 96-well plates and treated with borrelidin at concentrations ranging from 0.01 nM to 10 microM for 24-72 hours. Cell viability is assessed by MTT or CellTiter-Glo assays. Tube formation assays are performed: endothelial cells are seeded on Matrigel-coated plates and treated with borrelidin (0.1-10 nM). Tube formation is quantified after 6-18 hours by measuring tube length, branch points, and closed loops using image analysis. Apoptosis is assessed by caspase activity assays or Annexin V/PI staining. Cell cycle analysis is performed by flow cytometry.
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| Animal Protocol |
In vivo anti-angiogenic activity is evaluated in mouse models of tumor angiogenesis. Immunodeficient mice are implanted with tumor cells or Matrigel plugs containing VEGF and bFGF. Borrelidin is administered intraperitoneally or intravenously at doses ranging from 0.1-1 mg/kg daily. Tumor growth or angiogenesis is assessed by measuring tumor volume, hemoglobin content, or CD31 immunohistochemistry. For pharmacokinetic studies, blood samples are collected at various time points and drug concentrations are measured by LC-MS/MS.
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| ADME/Pharmacokinetics |
Borrelidin (C2₈H43NO₆, MW ~489.6) is a macrolide antibiotic with moderate lipophilicity. It is soluble in DMSO, ethanol, methanol, and other organic solvents. Pharmacokinetic properties are not extensively reported, but the compound has been used in mouse models for anti-angiogenic studies. The compound is typically administered parenterally. Half-life and bioavailability data are limited.
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| Toxicity/Toxicokinetics |
Borrelidin exhibits potent biological activity and should be handled with appropriate precautions. As an antibiotic and anti-angiogenic agent, it may have effects on protein synthesis and angiogenesis that could be toxic at higher doses. The compound is for research use only and not for human therapeutic use.
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| References |
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| Additional Infomation |
According to reports, borrethoxin has been found in Streptomyces coelicoflavus, Streptomyces heilongjiangensis and other organisms with available data.
Borrelidin is a macrolide antibiotic and selective inhibitor of threonyl-tRNA synthetase. It exhibits potent anti-angiogenic activity (IC₅0 = 0.8 nM) and induces apoptosis in endothelial tube-forming cells. The compound has anti-viral, anti-bacterial, anti-malarial, and anti-angiogenic properties. Anti-angiogenesis effects are mediated through distinct pathways involving ThrRS inhibition and caspase activation. Borrelidin is not an approved therapeutic agent; it is a research compound for studying angiogenesis, protein synthesis, and cancer biology. |
| Molecular Formula |
C28H43NO6
|
|---|---|
| Molecular Weight |
489.644129037857
|
| Exact Mass |
489.309
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| CAS # |
7184-60-3
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| PubChem CID |
6436801
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
710.3±60.0 °C at 760 mmHg
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| Melting Point |
143-145℃
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| Flash Point |
383.4±32.9 °C
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| Vapour Pressure |
0.0±5.1 mmHg at 25°C
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| Index of Refraction |
1.539
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| LogP |
4.31
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
35
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| Complexity |
827
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@H]1C[C@H](C[C@@H]([C@H](/C(=C\C=C\C[C@H](OC(=O)C[C@@H]([C@H](C1)C)O)[C@@H]2CCC[C@H]2C(=O)O)/C#N)O)C)C
|
| InChi Key |
OJCKRNPLOZHAOU-UGKRXNSESA-N
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| InChi Code |
InChI=1S/C28H43NO6/c1-17-12-18(2)14-20(4)27(32)21(16-29)8-5-6-11-25(22-9-7-10-23(22)28(33)34)35-26(31)15-24(30)19(3)13-17/h5-6,8,17-20,22-25,27,30,32H,7,9-15H2,1-4H3,(H,33,34)/b6-5+,21-8-/t17-,18+,19-,20-,22+,23+,24-,25-,27+/m0/s1
|
| Chemical Name |
(1R,2R)-2-[(2S,4E,6Z,8R,9S,11R,13S,15S,16S)-7-cyano-8,16-dihydroxy-9,11,13,15-tetramethyl-18-oxo-1-oxacyclooctadeca-4,6-dien-2-yl]cyclopentane-1-carboxylic acid
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
Ethanol :≥ 100 mg/mL (~204.23 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.11 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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: ≥ 2.5 mg/mL (5.11 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (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 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0423 mL | 10.2116 mL | 20.4232 mL | |
| 5 mM | 0.4085 mL | 2.0423 mL | 4.0846 mL | |
| 10 mM | 0.2042 mL | 1.0212 mL | 2.0423 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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