Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 9,000 | |||
10 mg | 在庫あり | ¥ 13,000 | |||
25 mg | 在庫あり | ¥ 22,500 | |||
50 mg | 在庫あり | ¥ 33,000 | |||
100 mg | 在庫あり | ¥ 53,500 | |||
200 mg | 在庫あり | ¥ 89,000 | |||
500 mg | 在庫あり | ¥ 148,500 |
説明 | Kobe0065 is a novel and effective small-molecule compound inhibiting Ras–Raf interaction by SBDD; shows potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
ターゲット&IC50 | C-Raf1 RBD:46 ± 13 μM(ki) |
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[1]. |
In vivo | Kobe0065 has antitumor activity. The compound-treated tumors show a prominent increase of apoptotic cells without any significant body weight loss[1]. |
キナーゼ試験 | 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. |
細胞研究 | 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) |
分子量 | 449.79 |
分子式 | C15H11ClF3N5O4S |
CAS No. | 436133-68-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 4.5 mg/mL (10 mM)), Heating is recommended.
DMSO: 20 mg/ml
You can also refer to dose conversion for different animals. 詳細
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Kobe0065 436133-68-5 Apoptosis GPCR/G Protein MAPK Raf Ras inhibit Inhibitor Kobe-0065 Kobe 0065 inhibitor