KKL-35 is a trans-translation tagging reaction inhibitor with an IC 50 of 0.9 μM.
性状
Solid
IC50 & Target[1][2]
IC50: 0.9 μM (trans-translation tagging reaction)
体外研究(In Vitro)
KKL-35 exhibits broad-spectrum antibiotic activity. KKL-35 prevents growth of B. anthracis and M. smegmatis with minimum inhibitory concentration (MIC) values of less than 6 μM. KKL-35 inhibit trans-translation at some step before proteolysis of tagged proteins. KKL-35 inhibits tagging of DHFR-ns. A large amount of untagged DHFR is produced in reactions with the highest concentrations of KKL-35, indicating that KKL-35 does not inhibit translation. KKL-35 prevents growth of WT S. flexneri with a MIC of 6 μM, and addition of KKL-35 to a growing culture of S. flexneri stops growth. In an S. flexneri strain expressing ArfA and deleted for ssrA, addition of KKL-35 has little effect on viability or growth rate. KKL-35 inhibits the growth of E. coli ?tolC, which is deficient in small molecule efflux, with an MIC of 0.3 μM.
体内研究(In Vivo)
Evidence suggest that the in vivo effects of KKL-35 are caused by inhibition of the release of nonstop translation complexes by trans-translation. KKL-35 inhibits trans-translation and prevents growth of S. flexneri strains that require trans-translation. The correlation between inhibition of trans-translation and growth is supported by genetic and pharmacological experiments showing that alternative mechanisms to release nonstop translation complexes relieve the growth suppression of KKL-35. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Ramadoss NS, et al. Small molecule inhibitors of trans-translation have broad-spectrum antibiotic activity. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):10282-7.
溶解度数据
In Vitro: DMSO : 6.25 mg/mL (19.67 mM; Need ultrasonic)配制储备液