kobe2602|cas 454453-49-7| DC Chem|Supplier|Price|Buy 

kobe2602|cas 454453-49-7| DC Chem|Supplier|Price|Buy

DC Chemicals Supply: kobe2602, Cas: 454453-49-7 ,Cat No. DC7444, Purity>98%, In stock.

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kobe2602|cas 454453-49-7, Synonym name: kobe 2602; kobe-2602, Chemical name:　, Molecule weight: 419.31, Molecule Formula: C14H9F4N5O4S

kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.

kobe2602 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; exhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 149 ± 55 μM.

IC50 value: 149 ± 55 uM (Ki) [1]

Target: Ras-Raf

These two compounds(Kobe0065 and Kobe2602), added to the culture medium at 2 and 20 μM, effectively reduced the amount of c-Raf-1 associated with H-Ras G12V in NIH 3T3 cells in a dose-dependent manner, indicating the inhibition of the cellular activity of Ras. A rough estimate of the IC50 value for the cellular Ras–Raf-binding inhibition was around 10 μM (Fig. 1B), which was not much different from the Ki values for the in vitro Ras–Raf-binding inhibition considering thequite low cellular concentration of Raf. A similar inhibitory effect was also observed with NIH 3T3 cells overexpressing K-Ras G12V. Both Kobe0065 and Kobe2602 at 20 μM efficiently inhibited the phosphorylation of MEK and ERK, downstream kinases of Raf in NIH 3T3 cells transiently expressing

H-Ras G12V, although the effect was slightly weaker than that of

2 μM sorafenib.