ECBN biosynthesis cluster Ani in the genome of the echinocandin B producer strain A. nidulans NRRL 8112. ECBN belongs to lipopeptide antifungal antibiotic bearing five types of direct precursor amino acids including proline, ornithine, tyrosine, threonine, and leucine. ECBN obtained by the fermentation of Aspergillus nidulans and Aspergillus rugulosus, is known as one of the natural cyclic hexapeptides that have a linoleoyl side chain, which inhibits a crucial enzyme in fungal cell wall biosynthesis, β-(1,3)-d-glucan synthase.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Enhancement of Echinocandin B Production by a UV- and Microwave-Induced Mutant of Aspergillus nidulans with Precursor- and Biotin-Supplying Strategy.
Hu ZC, et al. Appl Biochem Biotechnol. 2016 Aug;179(7):1213-26. PMID: 27039401.
Efficient bioconversion of echinocandin B to its nucleus by overexpression of deacylase genes in different host strains.
Shao L, et al. Appl Environ Microbiol. 2013 Feb;79(4):1126-33. PMID: 23220968.
BMS-5 is a Potent LIM kinase inhibitor (IC50 values are 7 and 8 nM for LIMK1 and LIMK2 respectively).Inhibits cofilin phosphorylation in MDA-MB-231 breast cancer cells. Reduces MDA-MB-231 tumor cell invasion in a 3D matrigel invasion assay.
BMS-3 is a potent inhibitor of LIMK1.LIM kinase 1 (LIMK1) activity is essential for cell migration and cell cycle progression.
E7046 is an orally bioavailable and specific EP4 antagonist, with IC50 of 13.5 nM and Ki of 23.14 nM, exhibiting anti-tumor activities.
PF-05175157 (Compound 9) is a potent Acetyl-CoA carboxylase (ACC1) inhibitor with IC50s of 23.5±1.1 nM (rat) and 27.0±2.7 nM (human).
Epacadostat (INCB024360) is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM and displays high selectivity over other related enzymes such as IDO2 or tryptophan 2,3-dioxygenase (TDO).
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