Ganfeborole hydrochloride (Synonyms: GSK656; GSK3036656; GSK070)

Name: Ganfeborole hydrochloride
Brand: MedChemExpress
SKU: HY-107775
Rating: 5.0 (3 reviews)

Cat. No.: HY-107775 Purity: 99.97%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

Ganfeborole hydrochloride Chemical Structure

CAS No. : 2131798-13-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 605	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 605	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1700	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2700	In-stock	Estimated Time of Arrival: December 31
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200 mg		Get quote

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Based on 3 publication(s) in Google Scholar

Other Forms of Ganfeborole hydrochloride:

Ganfeborole Get quote

3 Publications Citing Use of MCE Ganfeborole hydrochloride

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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.

IC₅₀ & Target

IC50: 0.2 μM (Mtb LeuRS)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	381 μM Compound: 23a; GSK656	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	[PMID: 28953378]

In Vitro

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.

In Vivo

Ganfeborole hydrochloride shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED₉₉ of 0.4 mg/kg^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

293.94

Formula

C₁₀H₁₄BCl₂NO₄

CAS No.

2131798-13-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

OB1O[C@H](CN)C2=C(Cl)C=CC(OCCO)=C21.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4021 mL	17.0103 mL	34.0205 mL
5 mM	0.6804 mL	3.4021 mL	6.8041 mL
10 mM	0.3402 mL	1.7010 mL	3.4021 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (292 KB) SDS (644 KB)

COA (251 KB) HNMR (156 KB) RP-HPLC (162 KB) LCMS (376 KB)

Handling Instructions (2659 KB)

References

[1]. Li X, et al. Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656). J Med Chem. 2017 Oct 12;60(19):8011-8026. [Content Brief]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Li X, et al. Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656). J Med Chem. 2017 Oct 12;60(19):8011-8026. [Content Brief]

Complete Stock Solution Preparation Table

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

Ganfeborole hydrochloride Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ganfeborole2131798-13-3GSK656 GSK3036656 GSK070GSK 656GSK-656GSK3036656GSK 3036656GSK-3036656GSK070GSK 070GSK-070BacterialInhibitorinhibitorinhibit

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Ganfeborole hydrochloride (Synonyms: GSK656; GSK3036656; GSK070)

Customer Review

Other Forms of Ganfeborole hydrochloride:

Ganfeborole hydrochloride Related Antibodies

3 Publications Citing Use of MCE Ganfeborole hydrochloride

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Ganfeborole hydrochloride Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Ganfeborole hydrochloride Related Classifications

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