化合物Kobe0065 T1876

Product Introduction
Bioactivity


英文名: Kobe0065

描述: Kobe0065 是一种新型 Ras-Raf 相互作用抑制剂，可完全抑制 H-Ras·GTP 与 c-Raf-1 RBD 的结合，Ki 值为 46±13 μM。

细胞实验: NIH 3T3 cells are transfected with pEF-BOS-HA-H-Ras(G12V) or an empty vector and treated with the 2 and 20 μM compound or the vehicle (DMSO) in the presence of 2% FBS for 1 h. Cell lysate is subjected to detection of c-Raf-1 coimmunoprecipitated with an anti-H-Ras antibody and total c-Raf-1 by Western blotting with an anti-c-Raf-1 antibody. Immunoprecipitated H-Ras(G12V) are detected by an anti-HA antibody.(Only for Reference)

激酶实验: Determination of lipase activity: For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean S.D. of triplicate determinations and representative for at least three independent experiments.

体外活性: 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[1].

体内活性: Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 4.5 mg/mL (10 mM))
DMSO : 20 mg/ml


关键字: inhibit | Inhibitor | Ras | Kobe-0065 | Kobe 0065 | Apoptosis | Kobe0065

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相关库: HIF-1 Signaling Pathway Compound Library | Glutamine Metabolism Compound Library | Membrane Protein-targeted Compound Library | Fluorochemical Library | Kinase Inhibitor Library | Inhibitor Library | GPCR Compound Library | PPI Inhibitor Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library

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