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

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

BPH-1358 free base (NSC50460 free base) 是一种有效的人 FPPSUPPS 抑制剂,IC50 值分别为 1.8 μM 和 110 nM,在体外对金黄色葡萄球菌的 MIC 值大约为 250 ng/mL。

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

BPH-1358 free base Chemical Structure

CAS No. : 801985-13-7

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生物活性

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 & Target

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

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

528.60

Formula

C32H28N6O2

CAS 号

801985-13-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [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.

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