Description
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.
Product information
CAS Number: 2131798-13-3
Molecular Weight: 293.94
Formula: C10H14BCl2NO4
Chemical Name: (3S)-3-(aminomethyl)-4-chloro-7-(2-hydroxyethoxy)-1,3-dihydro-2,1-benzoxaborol-1-ol hydrochloride
Smiles: Cl.NC[C@H]1OB(O)C2=C1C(Cl)=CC=C2OCCO
InChiKey: FUOKBESTQMGROA-DDWIOCJRSA-N
InChi: InChI=1S/C10H13BClNO4.ClH/c12-6-1-2-7(16-4-3-14)10-9(6)8(5-13)17-11(10)15;/h1-2,8,14-15H,3-5,13H2;1H/t8-;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 67.5 mg/mL (229.64 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
GSK656 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. GSK656 exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. GSK656 also exhibits EC50s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis.
In Vivo:
GSK656 shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED99 of 0.4 mg/kg.
Products are for research use only. Not for human use.
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