EHop-016 |
| Catalog No.GC10030 |
Inhibidor de la GTPasa Rac1/Rac3, potente y específico.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1380432-32-5
Sample solution is provided at 25 µL, 10mM.
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EHop-016 is a novel and specific inhibitor of Rac1 and Rac3 activity (IC50= 1.1 μm).
Rac is a member of the RAS superfamily of small GTPase. It functions in various cellular processes including regulation of secretory processes, membrane ruffles, cell polarization and phagocytosis of apoptotic cells etc. It is contributed to malignant progression.
Ehop-016 inhibited Rac activity in metastatic cancer cell MDA-MB-435 which overexpressed Rac and inhibited high endogenous Rac activity as well. In metastatic breast cancer cell MDA-MB-231, Ehop-016 blocked the Rac activity and reduced Rac-mediated lamelipodia formation. It also attenuated the effects of Rac downstream protein p21-activated kinase 1 and directed migration of metastatic cancer cells. [1]
In C3H/HeJ mice carrying KITD814V following overnight treatment of 2.5 μM EHop-016 or 25 μM NSC23766, EHop-016 reduced spleen size and PB counts thus significantly promoted the survival of leukemic mice compared with NSC23766. [2]
References:
1. Montalvo-Ortiz BL, Castillo-Pichardo L, Hernández E et al. Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J Biol Chem. 2012 Apr 13;287(16):13228-38.
2. Martin H, Mali RS, Ma P et al. Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest. 2013 Oct;123(10):4449-63.
| Kinase experiment [1]: | |
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Rac Activity Assays |
Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines. Cancer cells in culture medium (DMEM, 10% FBS, pH 7.5) are treated with vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Rac1 activity is determined using the G-LISA Rac1 activation assay kit. |
| Cell experiment [1]: | |
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Cell lines |
MDA-MB-435 and MDA-MB-231 metastatic cancer cells |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
0–10 μM for 24 h |
|
Applications |
EHop-016 inhibited Rac activity and reduced Rac-directed lamellipodia formation in both MDA-MB-435 and MDA-MB-231 metastatic cancer cells. Moreover, EHop-016 decreased Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed metastatic cancer cells migration. |
| Animal experiment [2]: | |
|
Animal models |
KITD814V-bearing mice model |
|
Dosage form |
2.5 μM; i.v. injection, for 45 days; |
|
Applications |
Treatment of KITD814V-bearing cells with EHop-016 significantly enhanced leukemic mice survival and delayed disease progression. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: 1Montalvo-Ortiz, B. L., Castillo-Pichardo, L., Hernandez, E., Humphries-Bickley, T., De la Mota-Peynado, A., Cubano, L. A., Vlaar, C. P. and Dharmawardhane, S. (2012) Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J Biol Chem. 287, 13228-13238 2Martin, H., Mali, R. S., Ma, P., Chatterjee, A., Ramdas, B., Sims, E., Munugalavadla, V., Ghosh, J., Mattingly, R. R., Visconte, V., Tiu, R. V., Vlaar, C. P., Dharmawardhane, S. and Kapur, R. (2013) Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest. 123, 4449-4463 | |
| Cas No. | 1380432-32-5 | SDF | |
| Chemical Name | 4-N-(9-ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine | ||
| Canonical SMILES | CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51 | ||
| Formula | C25H30N6O | M.Wt | 430.55 |
| Solubility | ≥ 25.6mg/mL in DMSO with gentle warming | Storage | Store at -20° C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3226 mL | 11.6131 mL | 23.2261 mL |
| 5 mM | 0.4645 mL | 2.3226 mL | 4.6452 mL |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3226 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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