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Usage

Uses

Used in Pharmaceutical Industry:
Kobe-2602 is used as a chemical intermediate for the preparation of pyrazolidine or pyrazole compounds that exhibit mild antimicrobial effects against various strains of bacteria. This makes it a valuable component in the development of new antimicrobial agents to combat bacterial infections.
Additionally, 2-[2,6-Dinitro-4-(trifluoromethyl)phenyl]-N-(4-fluorophenyl)hydrazinecarbothioamide, another chemical compound, is also used in the preparation of pyrazolidine or pyrazole compounds with similar antimicrobial properties, further expanding the range of applications for Kobe-2602 in the pharmaceutical industry.

Biological Activity

kobe2602 is a small-molecule inhibitor of ras with ki value of 149 μm [1].kobe2602 is a compound screened out by a computer-assisted search of about 160,000 compounds. it dose-dependently inhibited the binding of h-rasg12v to c-raf-1 in nih 3t3 cells with a rough ic50 value of 10 μm. 20 μm of kobe2602 effectively suppressed the phosphorylation of down-stream kinases of raf, including mek and erk. besides that, in nih 3t3 cells transfected with h-rasg12v, kobe2602 inhibited the colony formation with ic50 value of 1.4 μm. kobe2602 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 kobe2602 resulted in 40-50% inhibition of the tumor growth at dose of 80 mg/kg [1].

references

[1] shima f, yoshikawa y, ye m, et al. in silico discovery of small-molecule ras inhibitors that display antitumor activity by blocking the ras–effector interaction. proceedings of the national academy of sciences, 2013, 110(20): 8182-8187.