BPH-1358 free base  (Synonyms: NSC50460 free base)

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].

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

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

528.60

C₃₂H₂₈N₆O₂

801985-13-7

O=C(C1=CC=C(C2=CC=C(C(NC3=CC=CC(C4=NCCN4)=C3)=O)C=C2)C=C1)NC5=CC=CC(C6=NCCN6)=C5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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

  [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.  [Content Brief]