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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Parasite-Borrelidin
Borrelidin

Chemical Structure : Borrelidin

CAS No.: 7184-60-3

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Borrelidin (Treponemycin)

货号: PC-26820Not For Human Use, Lab Use Only.

Borrelidin is a small molecule nitrile-containing macrolide inhibitor of bacterial and eukaryal threonyl-tRNA synthetase (ThrRS), inhibits protein synthesis, also shows stage-specific growth inhibition for Plasmodium falciparum.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Borrelidin is a small molecule nitrile-containing macrolide inhibitor of bacterial and eukaryal threonyl-tRNA synthetase (ThrRS), inhibits protein synthesis, also shows stage-specific growth inhibition for Plasmodium falciparum.
Borrelidin potently inhibits the proliferation of ALL cell lines with IC50 of 50 ng/mL.
Borrelidin is able to increase the level of apoptosis and cause G(1) arrest in ALL cell lines.
Borrelidin also inhibits a cyclin-dependent kinase (CDK), Cdc28/Cln2, of Saccharomyces cerevisiae with IC50 of 24 uM.
Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively.

物理化学性质&存储条件

分子量 489.65
分子式 C28H43NO6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(1R,2R)-2-((2S,4E,6Z,8R,9S,11R,13S,15S,16S)-7-Cyano-8,16-dihydroxy-9,11,13,15-tetramethyl-18-oxooxacyclooctadeca-4,6-dien-2-yl)cyclopentane-1-carboxylic acid

参考文献

1. Habibi D, et al. Invest New Drugs. 2012 Aug;30(4):1361-70.

2. Tsuchiya E, et al. J Antibiot (Tokyo). 2001 Jan;54(1):84-90.

3. Aki Ishiyama, et al. J Antibiot (Tokyo). 2011 May;64(5):381-4.

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