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BPH-1358 free base

Names

[ CAS No. ]:
801985-13-7

[ Name ]:
BPH-1358 free base

Biological Activity

[Description]:

BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC50s of 1.8 μM and 110 nM, respectively, and is active against S. aureus in vitro (MIC ~250 ng/mL)[1][2].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Bacterial

[Target]

IC50: 1.8 μM (human bisphosphonate farnesyl diphosphate synthase)[1]; 100 nM (undecaprenyl diphosphate synthase)[2]


[In Vitro]

BPH-1358 is the most potent inhibitor of both E. coli UPPS (EcUPPS) as well as S. aureus UPPS (SaUPPS) with an IC50 of 110 nM. BPH-1358 against E. coli and S. aureus with EC50 of 300 nM and 290 nM, respectively[1].

[In Vivo]

BPH-1358 is active against S. aureus in vivo (20/20 mice survived in an i.p. infection model with a MRSA strain)[1].

[References]

[1]. Zhu W, et al. Antibacterial drug leads: DNA and enzyme multitargeting. J Med Chem. 2015 Feb 12;58(3):1215-27.

[2]. Liu YL, et al. Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries. ACS Med Chem Lett. 2015 Jan 29;6(3):349-54.

Chemical & Physical Properties

[ Molecular Formula ]:
C32H28N6O2

[ Molecular Weight ]:
528.60

Related Compounds