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Kobe0065

CAS No. : 436133-68-5

MCE 国际站：Kobe0065

产品活性：Kobe0065 是一种新颖的，有效的 Ras-Raf 相互作用抑制剂，能够完全抑制 H-Ras·GTP 与 c-Raf-1 RBD 的结合，K_i 值为 46±13 μM。

研究领域：GPCR/G Protein | Apoptosis

作用靶点：Ras | Apoptosis

In Vitro: Kobe0065-family compounds bind to Ras•GTP and exhibit antiproliferative activity toward cancer cells carrying the activated ras oncogenes. The compounds efficiently inhibit the interaction of Ras•GTP with their multiple effectors including Raf, PI3K, and RalGDS and a regulator/effector Sos and show rather broad binding specificity toward various Ras family small GTPases, which may account for their higher potency at the cellular level compared with that of the in vitro binding inhibition. The phosphorylation of downstream kinases MEK and ERK is effectively attenuated by 20 μM Kobe0065 and Kobe2602 in NIH3T3 cells transiently expressing H-RasG12V.

In Vivo: Kobe0065 and Kobe2602 exhibit antitumor activity on a xenograft of human colon carcinoma SW480 cells carrying the K-ras(G12V) gene by oral administration.

相关产品：Apoptosis Compound Library | GPCR/G Protein Compound Library | Glutamine Metabolism Compound Library | Ferroptosis Compound Library | Anti-Cancer Compound Library | Bioactive Compound Library Plus | MG-132 | LY294002 | Doxorubicin hydrochloride | Bafilomycin A1 | Paclitaxel | Y-27632 dihydrochloride | Sorafenib | SP600125 | Staurosporine | Angiotensin II human | 5-Fluorouracil | Trametinib | Acetylcysteine | MK-2206 dihydrochloride | Bortezomib | Tamoxifen | AMG-510 | Gemcitabine | Pexidartinib | 2-Deoxy-D-glucose | Temozolomide | Ruxolitinib | Verteporfin | Decitabine | BAY 11-7082 | Mdivi-1 | Etoposide | DAPT | Dasatinib

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