GSK-656

Research use only, not for human use.

GSK-656 (GSK-3036656, GSK656)?is a potent, highly selective,orally bioavailable Mtb Leucyl-tRNA synthetase (LeuRS) with IC50 of 0.2 uM.

GSK-656 (GSK-3036656, GSK656)?is a potent, highly selective,orally bioavailable Mtb Leucyl-tRNA synthetase (LeuRS) with IC50 of 0.2 uM; displays no significant activity for human mitochondrial LeuRS and human cytoplasmic LeuRS (IC50>100 uM); shows potent antitubercular activity (Mtb H37Rv IC50=0.08 uM) in vitro; exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models.Bacterial Infection.Phase 1 Clinical.

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.

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

GSK656 | GSK 656 | GSK3036656 | GSK-3036656

GPCR/G Protein

Antibacterial

Antibacterial

Infection

Bacterial Infection

2131798-13-3

293.935

C10H14BCl2NO4

>98% (HPLC)

DMSO : 67.5 mg/mL 229.64 mM

B1(C2=C(C=CC(=C2C(O1)CN)Cl)OCCO)O.Cl

(S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c]-[1,2]oxaborol-1(3H)-ol hydrochloride

(-20℃)

With Ice Pack

≥ 2 years