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Chemical Structure : EHop-016
CAS No.: 1380432-32-5
Catalog No.: PC-43223Not For Human Use, Lab Use Only.
EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 uM, which is 100-fold lower than for NSC23766, EHop-016 is specific for Rac1 and Rac3 at <5 uM.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $78 | In stock | |
| 25 mg | $128 | In stock | |
| 50 mg | $198 | In stock | |
| 100 mg | $298 | In stock | |
| 200 mg | Get quote | ||
| 1 g | Get quote |
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EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 uM, which is 100-fold lower than for NSC23766, EHop-016 is specific for Rac1 and Rac3 at <5 uM.
EHop-016 also inhibits the close homolog Cdc42 at higher concentrations; inhibits Rac activity in the MDA-MB-435 metastatic cancer cells that overexpress Rac and exhibits high endogenous Rac activity.
EHop-016 inhibits the association of Vav2 with a nucleotide-free Rac1(G15A) in MDA-MB-435 cells.
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, decreases Rac downstream effects of PAK1 activity and directed migration of metastatic cancer cells.
EHop-016 inhibits mammary tumor growth and metastasis in nude mouse model.
| M.Wt | 430.5453 | |
| Formula | C25H30N6O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
DMSO: ≥ 32 mg/mL |
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| Chemical Name/SMILES |
2,4-Pyrimidinediamine, N4-(9-ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]- |
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1. Montalvo-Ortiz BL, et al. J Biol Chem. 2012 Apr 13;287(16):13228-38.
2. Dharmawardhane S, et al. Enzymes. 2013;33 Pt A:117-46.
3. Martin H, et al. J Clin Invest. 2013 Oct;123(10):4449-63.
4. Castillo-Pichardo L, et al. Transl Oncol. 2014 Oct 24;7(5):546-55.
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