Borrelidin

Borrelidin (Treponemycin) is a bacterial and eukaryal threonyl-tRNA synthetase inhibitor which is a nitrile-containing macrolide antibiotic isolated from Streptomyces rochei[1]. Borrelidin is an inhibitor of Cdc28/Cln2 of the budding yeast, with an IC50 of 24 μM[2]. Borrelidin is a potent angiogenesis inhibitor, with an IC50 of 0.8 nM. Borrelidin induces apoptosis in the tube-forming cells[3]. Borrelidin has strong antimalarial activities, with IC50s of 1.9 nM and 1.8 nM against K1 and FCR3 strains of Plasmodium falciparum, respectively[4].

Product Specifications

CAS Number

[7184-60-3]

Product Name Alternative

Treponemycin

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Antibiotic; Apoptosis; CDK; Parasite

Type

Natural Products

Related Pathways

Anti-infection; Apoptosis; Cell Cycle/DNA Damage

Applications

COVID-19-anti-virus

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/borrelidin.html

Purity

99.80

Solubility

Ethanol : ≥ 100 mg/mL

Smiles

O=C([C@H]1[C@H]([C@H](C/C=C/C=C(C#N)\[C@H](O)[C@@H](C)C[C@H](C)C[C@H](C)C[C@H](C)[C@@H](O)C2)OC2=O)CCC1)O

Molecular Formula

C28H43NO6

Molecular Weight

489.64

Precautions

H302, H315, H319, H335

References & Citations

[1]Habibi D, et al. Borrelidin, a small molecule nitrile-containing macrolide inhibitor of threonyl-tRNA synthetase, is a potent inducer of apoptosis in acute lymphoblastic leukemia. Invest New Drugs. 2012 Aug;30 (4) :1361-70.|[2]Tsuchiya E, et al. Borrelidin inhibits a cyclin-dependent kinase (CDK), Cdc28/Cln2, of Saccharomyces cerevisiae. J Antibiot (Tokyo) . 2001 Jan;54 (1) :84-90.|[3]Wakabayashi T, et al. Borrelidin is an angiogenesis inhibitor; disruption of angiogenic capillary vessels in a rat aorta matrix culture model. J Antibiot (Tokyo) . 1997 Aug;50 (8) :671-6.|[4]Otoguro K, et al. In vitro and in vivo antimalarial activities of a non-glycosidic 18-membered macrolide antibiotic, borrelidin, against drug-resistant strains of Plasmodia. J Antibiot (Tokyo) . 2003 Aug;56 (8) :727-9.