Overview

  • Product name

    EHop-016, Rac GTPase inhibitor
  • Description

    Specific Rac GTPase inhibitor
  • Biological description

    Specific Rac GTPase inhibitor. Analog of NSC-23766 (ab142161). Approximately 100-fold more potent against Rac (IC50 = 1.1 μM) than NSC-23766. Specific for Rac1 and Rac3 at concentrations of ≤5 μM. At higher concentrations (10μM) inhibits the the related Rho GTPase Cdc42. Also inhibits the activity of the Rac downstream effector p21-activated kinase (PAK), lamellipodia extension, and cell migration in metastatic cancer cells.

  • Purity

    > 98%
  • CAS Number

    1380432-32-5

Properties

  • Chemical name

    N4-(9-Ethylcarbazol-3-yl)-2-N2-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine
  • Molecular weight

    430.55
  • Molecular formula

    C25H30N6O
  • PubChem identifier

    51031035
  • Storage instructions

    Shipped at 4°C. Store at -20°C. Store In the Dark. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 100 mM
  • 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

    CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51
  • Source

    Synthetic

References

This product has been referenced in:

  • Castillo-Pichardo L  et al. The Rac Inhibitor EHop-016 Inhibits Mammary Tumor Growth and Metastasis in a Nude Mouse Model. Transl Oncol 7:546-55 (2014). Read more (PubMed: 25389450) »
  • Dharmawardhane S  et al. Development of EHop-016: a small molecule inhibitor of Rac. Enzymes 33 Pt A:117-46 (2013). Read more (PubMed: 25033803) »
  • Montalvo-Ortiz BL  et al. Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J Biol Chem 287:13228-38 (2012). Read more (PubMed: 22383527) »

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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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