Name | KKL-35 |
Synonyms | SRJ-23 KKL-35 KKL-35(KKL 35 4-Chloro-N-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-benzamide Benzamide, 4-chloro-N-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]- |
CAS | 865285-29-6 |
Molecular Formula | C15H9ClFN3O2 |
Molar Mass | 317.7 |
Solubility | DMSO |
Appearance | powder |
Color | white to beige |
Storage Condition | Sealed in dry,2-8°C |
In vitro study | 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. |
In vivo study | 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. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.148 ml | 15.738 ml | 31.476 ml |
5 mM | 0.63 ml | 3.148 ml | 6.295 ml |
10 mM | 0.315 ml | 1.574 ml | 3.148 ml |
5 mM | 0.063 ml | 0.315 ml | 0.63 ml |
biological activity | KKL-35 inhibition of trans-translation tagging reaction with IC50 of 0.9 μm. It has broad-spectrum antibiotic activity. |
Target | IC50: 0.9 µm (trans -translation tagging reaction) |