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Description: Rac inhibitor
Chemical Name: N4-(9-Ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-2,4-pyrimidinediamine
Purity: ≥98% (HPLC)
Biological Activity for EHop 016
EHop 016 is a Rac inhibitor (IC50 = 1.1 μM). Exhibits some selectivity for Rac1 and Rac3 over Cdc42. Blocks the interaction of Rac with guanine nucleotide exchange factor Vav2 in breast cancer cell lines expressing high levels of Rac activity and inhibits activity of Rac downstream effector PAK1. Also inhibits mammary tumor growth and metastasis in mice.
Compound Libraries for EHop 016
EHop 016 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for EHop 016
| M. Wt | 430.55 |
| Formula | C25H30N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1380432-32-5 |
| PubChem ID | 51031035 |
| InChI Key | AFTZZRFCMOAFCR-UHFFFAOYSA-N |
| Smiles | CCN1C2=CC=C(NC3=NC(NCCCN4CCOCC4)=NC=C3)C=C2C5=CC=CC=C51 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for EHop 016
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 21.53 | 50 |
Preparing Stock Solutions for EHop 016
The following data is based on the product molecular weight 430.55. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.65 mL | 23.23 mL | 46.45 mL |
| 2.5 mM | 0.93 mL | 4.65 mL | 9.29 mL |
| 5 mM | 0.46 mL | 2.32 mL | 4.65 mL |
| 25 mM | 0.09 mL | 0.46 mL | 0.93 mL |
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Product Datasheets for EHop 016
References for EHop 016
References are publications that support the biological activity of the product.
Castillo-Pichardo et al (2014) The Rac inhibitor EHop-016 inhibits mammary tumor growth and metastasis in a nude mouse model. Transl.Oncol. 7 546 PMID: 25389450
Montalvo-Ortiz et al (2012) Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J.Biol.Chem. 287 13228 PMID: 22383527
If you know of a relevant reference for EHop 016, please let us know.
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Keywords: EHop 016, EHop 016 supplier, EHop016, Rac, inhibitors, inhibits, Vav2, GEFs, guanine, nucleotide, exchange, factors, Rac1, Rac3, Rho, 6248, Tocris Bioscience
1 Citation for EHop 016
Citations are publications that use Tocris products. Selected citations for EHop 016 include:
Ginam et al (2021) β2-adrenergic receptor regulates ER-mitochondria contacts. Sci Rep 11 21477 PMID: 34728663
Do you know of a great paper that uses EHop 016 from Tocris? Please let us know.
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