EHOP016
EHop-016
CAS: 1380432-32-5
Molecular Formula: C25H30N6O
EHOP016 - Names and Identifiers
EHOP016 - Physico-chemical Properties
| Molecular Formula | C25H30N6O |
| Molar Mass | 430.55 |
| Density | 1.27 |
| Boling Point | 633.9±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO, not in water |
| Appearance | powder |
| Color | white to beige |
| pKa | 7.30±0.10(Predicted) |
| Storage Condition | 2-8°C |
| MDL | MFCD23143628 |
| Use | EHop-016 is an effective and selective inhibitor of Rac GTPase Rac1 and Rac3. EHop-016 inhibited Rac1 activity in MDA-MB-435 cells with IC50 of 1.1 μM. EHop-016 inhibit Vav2 interaction with Rac,Rac-activated PAK1, lamellar lipoprotein formation and cell migration. |
| In vitro study | EHop-016 (1-10 μM; 24 hours; MDA-MB-435 cells) treatment inhibits Rac1 and Rac3 activity. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2, EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A) . EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells. EHop-016 affectes cell viability by down-regulating Akt and Jun kinase activities and c-Myc and Cyclin D expression, as well as increasing caspase 3/7 activities in metastatic cancer cells. Western Blot Analysis Cell Line: MDA-MB-435 cells Concentration: 1 μM, 2 μM, 4 μM, 5 μM, 10 μM Incubation Time: 24 hours Result: The activity Rac3 was inhibited by 58%. |
| In vivo study | EHop-016 (10-25 mg/kg; intraperitoneal injection; 3 times a week; for 55 days; nu/nu mice) treatment significantly reduces mammary fat pad tumor growth, metastasis, and angiogenesis. Animal Model: Female athymic nu/nu mice (4-5 weeks old) injected with GFP-MDA-MB-435 cells Dosage: 10 mg/kg, 25 mg/kg Administration: Intraperitoneal injection; 3 times a week; for 55 days Result: Significantly reduced mammary fat pad tumor growth, metastasis, and angiogenesis. |
EHOP016 - Risk and Safety
| WGK Germany | 3 |
EHOP016 - Reference
| Reference Show more | 1: Martin H, Mali RS, Ma P, Chatterjee A, Ramdas B, Sims E, Munugalavadla V, Ghosh J, Mattingly RR, Visconte V, Tiu RV, Vlaar CP, Dharmawardhane S, Kapur R. Pak and Rac GTPases promote oncogenic KIT-induced neoplasms. J Clin Invest. 2013 Oct 1;123(10):4449-63. doi: 10.1172/JCI67509. Epub 2013 Sep 16. PubMed PMID: 24091327; PubMed Central PMCID: PMC3784531. 2: Dharmawardhane S, Hernandez E, Vlaar C. Development of EHop-01 6: a small molecule inhibitor of Rac. Enzymes. 2013;33 Pt A:117-46. doi: 10.1016/B978-0-12-416749-0.00006-3. Epub 2013 Aug 8. Review. PubMed PMID: 25033803. 3: Montalvo-Ortiz BL, Castillo-Pichardo L, Hernández E, Humphries-Bickley T, De la Mota-Peynado A, Cubano LA, Vlaar CP, Dharmawardhane S. Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J Biol Chem. 2012 Apr 13;287(16):13228-38. doi: 10.1074/jbc.M111.334524. Epub 2012 Mar 1. PubMed PMID: 22383527; PubMed Central PMCID: PMC3339933. |
EHOP016 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.323 ml | 11.613 ml | 23.226 ml |
| 5 mM | 0.465 ml | 2.323 ml | 4.645 ml |
| 10 mM | 0.232 ml | 1.161 ml | 2.323 ml |
| 5 mM | 0.046 ml | 0.232 ml | 0.465 ml |
Last Update：2024-01-02 23:10:35
EHOP016 - Reference Information
| biological activity | EHop-016 is an effective selective Rac GTPase Rac1 and Rac3 inhibitors. EHop-016 inhibited Rac1 activity in MDA-MB-435 cells with IC50 of 1.1 μM. EHop-016 inhibit Vav2 interaction with Rac,Rac-activated PAK1, lamellar lipoprotein formation and cell migration. |
| in vitro study | EHop-016 (1-10μM; 24 hours; MDA-MB-435 cells) treatment inhibits Rac1 and Rac3 activity. At higher concentrations, EHop-016 inhibits the close homolog Cdc42. In MDA-MB-435 cells that demonstrate high active levels of the Rac GEF Vav2, EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A) . EHop-016 also inhibits the Rac activity of MDA-MB-231 metastatic breast cancer cells and reduces Rac-directed lamellipodia formation in both cell lines. EHop-016 decreases Rac downstream effects of PAK1 (p21-activated kinase 1) activity and directed migration of metastatic cancer cells. EHop-016 affectes cell viability by down-regulating Akt and Jun kinase activities and c-Myc and Cyclin D expression, as well as increasing caspase 3/7 activities in metastatic cancer cells. Western Blot Analysis Cell Line: MDA-MB-435 cells Concentration: 1 μ m, 2 μ m, 4 μ m, 5 μ m, 10 μ m Incubation time: 24 hours result: the activity Rac3 was inhibited by 58%. |
| Cell Line: | MDA-MB-435 cells |
| Concentration: | 1 μM, 2 μM, 4 μM, 5 μM, 10 μM |
| Incubation Time: | 24 hours |
| Result: | The activity Rac3 was inhibited by 58%. Significantly reduced mammary fat pad tumor growth, metastasis, and angiogenesis. |
| in vivo study | EHop-016 (10-25 mg/kg; intraperitoneal injection; 3 times a week; for 55 days; nu/nu mice) treatment significantly reduces mammary fat pad tumor growth, metastasis, and angiogenesis. Animal Model: Female athymic nu/nu mice (4-5 weeks old) injected with GFP-MDA-MB-435 cells Dosage: 10 mg/kg, 25 mg/kg Administration: Intraperitoneal injection; 3 times a week; For 55 days Result: Significantly reduced mammary fat pad tumor growth, metastasis, and angiogenesis. |
| Animal Model: | Female athymic nu/nu mice (4-5 weeks old) injected with GFP-MDA-MB-435 cells |
| Dosage: | 10 mg/kg, 25 mg/kg |
| Administration: | Intraperitoneal injection; 3 times a week; for 55 days |
Last Update：2024-04-09 15:16:37
Supplier List
Spot supply
Product Name: EHop-016 Visit Supplier Webpage Request for quotationCAS: 1380432-32-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: EHop-016 Visit Supplier Webpage Request for quotationCAS: 1380432-32-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History