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首页-小分子抑制剂&激动剂-Others-Small GTPase-EHop-016
EHop-016

Chemical Structure : EHop-016

CAS No.: 1380432-32-5

EHop-016 (Ehop 016)

货号: 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.

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10 mg ¥780 In stock
25 mg ¥1280 In stock
50 mg ¥1980 In stock
100 mg ¥2980 In stock
200 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 430.5453
分子式 C25H30N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

2,4-Pyrimidinediamine, N4-(9-ethyl-9H-carbazol-3-yl)-N2-[3-(4-morpholinyl)propyl]-

参考文献

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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