Product nameKobe0065, H-Ras-c-Raf1 interaction inhibitor
DescriptionSmall molecule inhibitor of the H-Ras-c-Raf1 interaction
Kobe0065 is small molecule inhibitor of the H-Ras-c-Raf interaction. It competitively inhibits the binding of H-Ras•GTD to c-Raf1 RBD with an IC50 of 46 μM. Exhibits antiproliferative activity in xenografts of SW480 colon carcinoma cells carrying the K-rasG12V gene. Inhibits anchorage-depoendent and independent growth and induces apotosis of NIH/3T3 cells transformed with K-rasG12V. Growth inhibition is accompanied by the down regulaton MEK/ERK, Akt, RalA, and Sos suggesting Kobe0065 blocks the interaction of H-Ras•GTp with mutiple effectors.
Storage instructionsShipped at 4°C. Store at +4°C short term (1-2 weeks). Store at -20°C long term. It is important to note that this is air sensitive and impurities can occur as a result of air oxidation. Store In the Dark. Store under desiccating conditions.
DMSO 89 mg/mL (197.87 mM)
Ethanol 13 mg/mL (28.9 mM)
Insoluble in water
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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This product has been referenced in:
- Yoshikawa Y et al. Ras inhibitors display an anti-metastatic effect by downregulation of lysyl oxidase through inhibition of the Ras-PI3K-Akt-HIF-1a pathway. Cancer Lett 410:82-91 (2017). Read more (PubMed: 28951129) »
- Shima F et al. In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction. Proc Natl Acad Sci U S A 110:8182-7 (2013). Read more (PubMed: 23630290) »
- Shima F et al. Discovery of small-molecule Ras inhibitors that display antitumor activity by interfering with Ras·GTP-effector interaction. Enzymes 34 Pt. B:1-23 (2013). Read more (PubMed: 25034098) »