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GSK932121

Chemical Structure : GSK932121

CAS No.: 958457-44-8

GSK932121 (GSK-932121)

Catalog No.: PC-20294Not For Human Use, Lab Use Only.

GSK932121 is a potent, selective inhibitor of P. falciparum cytochrome bc1 with IC50 of 7 nM, binds to Qi site of cytochrome bc1 and shows potent antimalarial activity in vitro and in vivo.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GSK932121 is a potent, selective inhibitor of P. falciparum cytochrome bc1 with IC50 of 7 nM, binds to Qi site of cytochrome bc1 and shows potent antimalarial activity in vitro and in vivo.
GSK932121 shows weak inhibition for cytochrome bc1 from HEK293 cells with IC50 of 400 nM (57-fold selectivity).
GSK932121 displays potent antimalarial activity against Plasmodium falciparumin vitro (P. falciparum 3D7A, IC50=6 nM, whole cell assay).
GSK932121 is potent against P. falciparum Pf3D70087/N9 as pyrimethamine in both HM-β2 mnull mice (ED90=0.6 mg/kg) and HM-IL2Rγnull mice (ED90=0.6 mg/kg).

Physicochemical Properties

M.Wt 425.79
Formula C20H15ClF3NO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-chloro-6-(hydroxymethyl)-2-methyl-5-(4-(4-(trifluoromethoxy)phenoxy)phenyl)pyridin-4(1H)-one

References

1. Bueno JM, et al. Future Med Chem. 2012 Dec;4(18):2311-23.

2. Capper MJ, et al. Proc Natl Acad Sci U S A. 2015 Jan 20;112(3):755-60.

3. María Belén Jiménez-Díaz, et al. Antimicrob Agents Chemother. 2009 Oct;53(10):4533-6.

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