Borrelidin | Threonyl-tRNA synthetase inhibitor

Chemical Structure : Borrelidin

CAS No.: 7184-60-3

Borrelidin (Treponemycin)

Catalog No.: PC-26820Not For Human Use, Lab Use Only.

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Biological Activity

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.

Physicochemical Properties

M.Wt	489.65
Formula	C28H43NO6
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	(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

References

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.

Borrelidin (Treponemycin)

Biological Activity

Physicochemical Properties

References

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