Ganfeborole hydrochloride
Based on 5 publication(s) in Google Scholar
Ganfeborole hydrochloride (GSK656) is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 2131798-13-3
- Formula: C10H14BCl2NO4
- Molecular Weight:293.94
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ganfeborole hydrochloride
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Biological Activity
IC50: 0.2 μM (Mtb LeuRS)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
381 μM
Compound: 23a; GSK656
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Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo assay
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[PMID: 28953378] |
Ganfeborole hydrochloride is highly selective inhibitor for Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM, and shows IC50s of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. Ganfeborole hydrochloride exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. Ganfeborole hydrochloride also exhibits EC50s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2131798-13-3
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Appearance Solid
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Molecular Weight 293.94
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Formula C10H14BCl2NO4
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Color Off-white to light yellow
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SMILES
OB1O[C@H](CN)C2=C(Cl)C=CC(OCCO)=C21.[H]Cl
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Synonyms
GSK656; GSK3036656; GSK070
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nat Nanotechnol
Nanofibrous supramolecular peptide hydrogels for controlled release of small-molecule drugs and biologics. [Abstract]2025 Oct;20(10):1502-1513. PMID: 40931056 -
Antimicrob Agents Chemother
A Novel Leucyl-tRNA Synthetase Inhibitor, MRX-6038, Expresses Anti-Mycobacterium abscessus Activity In Vitro and In Vivo. [Abstract]2022 Sep 20;66(9):e0060122. PMID: 35969055 -
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ACS Chem Biol
Investigate Natural Product Indolmycin and the Synthetically Improved Analogue Toward Antimycobacterial Agents. [Abstract]2022 Jan 21;17(1):39-53. PMID: 34908399 -
Solvent & Solubility
DMSO : 67.5 mg/mL (229.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
HepG2 (HB-8065) cells are cultured with fresh medium (essential minimum Eagle medium, EMEM, supplemented with 5% fetal calf serum and 2 mM l-glutamine) the day before subculturing the plates. On the day of the assay, cells (10 000 cells/well) are seeded in a black 96-well collagen coated microplate with clear bottom, except in column 11, which is dispensed only 100 mL of culture medium. Stock solution from GSK656 is prepared in 100% DMSO. Ten serial 1:2 dilutions are prepared of GSK656, and finally, a 1:200 dilution is made, in medium, to achieve a final concentration of 0.5% of DMSO. Resazurin tablets are dissolved in phosphate buffer saline at a concentration of 0.0042%. After 24 h of incubation of the cells (37°C, 5% CO2, 95% relative humidity), a volume of 150 μL of culture medium containing the appropriate test concentrations of GSK656 dilutions is added to cells in two replicates. Only 150 μL of 0.5% DMSO is added as blank control. Then, cells are exposed to GSK656 for 48 h. After that, medium is removed and resazurin solution is added to each well and incubated for further 1.5 h. Fluorescence is measured at an excitation wavelength of 515 nm and an emission wavelength of 590 nm in a Microplate reader 1420 Multilabel HTS counter, Victor 2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Specific pathogen-free, 8- to 10-week-old female C57BL/6 mice are allowed to acclimate for 1 week. In brief, mice are intratracheally infected with 100 000 CFU/mouse of M. tuberculosis H37Rv. GSK656 is administered for 8 consecutive days starting 1 day after infection. For the chronic assay, mice are intratracheally infected with 100 CFU/mouse and GSK656 administered daily (7 days a week) for 8 consecutive weeks starting 6 weeks after infection. Lungs are harvested 24 h after the last administration, and all lung lobes are aseptically removed, homogenized, and frozen. Homogenates are plated onto 10% OADC-Middlebrook 7H11 medium and incubated for 21 days at 37°C. GSK656 is administered by intravenous route at 5 mg/kg single dose in saline and by oral gavage at 30 mg/kg single dose in 1% methylcellulose (1% MC). For iv route aliquots of 15 μL of blood are taken from the lateral tail vein by puncture from each mouse (n = 3) at 5, 15, and 30 min and 1, 2, 4, 8, and 24 h postdose; for oral route aliquots of 15 μL of blood are taken from the lateral tail vein by puncture from each mouse (n = 3) at 15, 30, and 45 min and 1, 2, 4, 8, and 24 h postdose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (292 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4021 mL | 17.0103 mL | 34.0205 mL | 85.0514 mL |
| 5 mM | 0.6804 mL | 3.4021 mL | 6.8041 mL | 17.0103 mL | |
| 10 mM | 0.3402 mL | 1.7010 mL | 3.4021 mL | 8.5051 mL | |
| 15 mM | 0.2268 mL | 1.1340 mL | 2.2680 mL | 5.6701 mL | |
| 20 mM | 0.1701 mL | 0.8505 mL | 1.7010 mL | 4.2526 mL | |
| 25 mM | 0.1361 mL | 0.6804 mL | 1.3608 mL | 3.4021 mL | |
| 30 mM | 0.1134 mL | 0.5670 mL | 1.1340 mL | 2.8350 mL | |
| 40 mM | 0.0851 mL | 0.4253 mL | 0.8505 mL | 2.1263 mL | |
| 50 mM | 0.0680 mL | 0.3402 mL | 0.6804 mL | 1.7010 mL | |
| 60 mM | 0.0567 mL | 0.2835 mL | 0.5670 mL | 1.4175 mL | |
| 80 mM | 0.0425 mL | 0.2126 mL | 0.4253 mL | 1.0631 mL | |
| 100 mM | 0.0340 mL | 0.1701 mL | 0.3402 mL | 0.8505 mL |
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