GSK656 HCl (GSK3036656, GSK070)

This product is for research use only, not for human use. We do not sell to patients.

For small sizes, please check our retail website as below: www.invivochem.com

Size	Price	Stock
100mg	$2750	To Be Confirmed
200mg	$4125	To Be Confirmed
500mg	$6950	To Be Confirmed

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Cat #: V3594 CAS #: 2131798-13-3 Purity ≥ 98%

Description: GSK656 (GSK-3036656 and GSK-070) is a novel and potent antitubercular agent which acts as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM. There is an urgent need to develop new and safer antitubercular agents that possess a novel mode of action. GSK3036656 (abbreviated as GSK656) shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). Additionally, it is highly selective for the Mtb LeuRS enzyme with IC50 of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. In addition, it exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads. This compound has been progressed to clinical development for the treatment of tuberculosis.

References: 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.

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Physicochemical and Storage Information
Protocol
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Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	293.935
Molecular Formula	C10H14BCl2NO4
CAS No.	2131798-13-3
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
SMILES Code	OB1O[C@H](CN)C2=C(Cl)C=CC(OCCO)=C12.[H]Cl
Synonyms	GSK3036656; GSK-3036656; GSK 3036656; GSK070; GSK-070; GSK 070; GSK656; GSK-656; GSK 656; GSK656 HCl. GSK656 hydrochlorid

Protocol	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.
Protocol	In Vivo	Ganfeborole hydrochloride shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED99 of 0.4 mg/kg.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	3.4021 mL	17.0106 mL	34.0211 mL	68.0423 mL
5mM	0.6804 mL	3.4021 mL	6.8042 mL	13.6085 mL
10mM	0.3402 mL	1.7011 mL	3.4021 mL	6.8042 mL
20mM	0.1701 mL	0.8505 mL	1.7011 mL	3.4021 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(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.