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Kobe0065, CAS NO.436133-68-5
- FOB Price: USD: 1.00-1.00 /Gram Get Latest Price
- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- Kobe0065,
- Kobe 0065;Kobe0065;Kobe-0065;N-(3-Chloro-4-Methylphenyl)-2-[2,6-dinitro-4-(trifluoroMethyl)phenyl]-hydrazinecarbothioaMide;Kobe-0065 N-(3-Chloro-4-methylphenyl)-2-[2,6-dinitro-4-(trifluoromethyl)pheny
- 436133-68-5
Quick Details
- ProName: Kobe0065,
- CasNo: 436133-68-5
- Molecular Formula: C15H11ClF3N5O4S
- Appearance: white powder
- Application: CAS：436133-68-5；
- DeliveryTime: 2 months
- PackAge: 100g,500g,1kg,25kg/drum
- Port: shang hai
- ProductionCapacity: 1000 Gram/Week
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
Kobe0065 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 46 ± 13 μM.
IC50 value: 46 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