436133-68-5

Usage

Uses

Used in Pharmaceutical Industry:
Kobe-0065 is used as an intermediate compound for the synthesis of pyrazolidine or pyrazole compounds. These compounds are known for their mild antimicrobial effects against various strains of bacteria, making them valuable in the development of new antimicrobial drugs.
Used in Chemical Synthesis:
Kobe-0065 serves as a key building block in the preparation of various chemical compounds with potential applications in different fields. Its unique structure allows for further modification and functionalization, enabling the creation of new molecules with specific properties and uses.
Used in Research and Development:
In the realm of scientific research, Kobe-0065 can be employed as a starting material or a reference compound for studying the structure-activity relationships of related molecules. This can help researchers understand the underlying mechanisms of action and guide the design of more effective and targeted compounds.

Biological Activity

kobe0065 is a small-molecule inhibitor of ras with ki value of 46 μm for the binding of h-ras.gtp to c-raf-1 [1].kobe0065 is a compound screened out by an in silico screen method as a potent inhibitor of the ras–raf interaction. it showed favorite efficacy to inhibit the binding of m-ras.gtp and h-ras.gtp to the ras-binding domain of c-raf-1. kobe0065 also dose-dependently inhibited the binding of h-rasg12v to c-raf-1 in nih 3t3 cells with a rough ic50 value of 10 μm. besides that, 20 μm of kobe0065 effectively suppressed the phosphorylation of down-stream kinases of raf, including mek and erk. in nih 3t3 cells transfected with h-rasg12v, kobe0065 inhibited the colony formation with ic50 value of 0.5 μm. kobe0065 also showed effect on other cancer cells carrying activated ras oncogenes, such as panc-1(k-rasg12v), ht1080 (n-rasq61l) and hct116 (h-rasg13d). moreover, in mice bearing sw480 xenografts, administration of kobe0065 resulted in 40-50% inhibition of the tumor growth at dose of 80 mg/kg. this effect turned to be more distinct when the dose was up to 160 mg/kg [1].