Kobe0065, H-Ras-c-Raf1 interaction inhibitor (ab235574)

Overview

  • Product name

    Kobe0065, H-Ras-c-Raf1 interaction inhibitor
  • Description

    Small molecule inhibitor of the H-Ras-c-Raf1 interaction
  • Biological description

    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.

  • Purity

    > 98%
  • CAS Number

    436133-68-5
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-(3-chloro-4-methylphenyl)-2-(2,6-dinitro-4-(trifluoromethyl)phenyl)hydrazinecarbothioamide

  • Molecular weight

    449.79
  • Molecular formula

    C15H11ClF3N5O4S
  • PubChem identifier

    3827663
  • Storage instructions

    Shipped 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.
  • Solubility overview

    DMSO 89 mg/mL (197.87 mM)

    Ethanol 13 mg/mL (28.9 mM)

    Insoluble in water

  • Handling

    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.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CC1=C(C=C(C=C1)NC(=S)NNC2=C(C=C(C=C2[N+](=O)[O-])C(F)(F)F)[N+](=O)[O-])Cl
  • Source

    Synthetic

References

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) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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