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EHop-016 是一种特异性 Rac GTPase 抑制剂,对 MDA-MB-231 和 MDA-MB-435 细胞中的 Rac1 的 IC50 为 1.1 μM,也可抑制Rac3 。它还抑制 Vav2 与 Rac,Rac 激活的 PAK1 相互作用,片状脂蛋白形成和细胞迁移。
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EHop-016 是一种特异性 Rac GTPase 抑制剂,对 MDA-MB-231 和 MDA-MB-435 细胞中的 Rac1 的 IC50 为 1.1 μM,也可抑制Rac3 。它还抑制 Vav2 与 Rac,Rac 激活的 PAK1 相互作用,片状脂蛋白形成和细胞迁移。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 159 | 现货 | |
5 mg | ¥ 343 | 现货 | |
10 mg | ¥ 551 | 现货 | |
25 mg | ¥ 1,080 | 现货 | |
50 mg | ¥ 1,650 | 现货 | |
100 mg | ¥ 2,460 | 现货 | |
200 mg | ¥ 3,630 | 现货 | |
500 mg | ¥ 5,790 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 343 | 现货 |
产品描述 | EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3. |
靶点活性 | Rac1:1.1 μM |
体外活性 | EHop-016使患有KITD814V细胞的白血病小鼠存活率得到显著提高. |
体内活性 | 在MDA-MB-435细胞中,EHop-016(2-5 μM)抑制活性VAV2与Rac1(G15A)突变体融合蛋白的结合,并使Rac调控的细胞功能减少,包括板状伪足形成和细胞迁移。由于代偿机制,EHop-016对Rac的抑制增加了与之密切相关的Rho GTPase RhoA活性。此外,EHop-016抑制MDA-MB-435细胞的细胞活性(IC50:10 μM)。 EHop-016还抑制了来自SM和AML患者的细胞中KITD814V诱导的生长。 |
激酶实验 | Rac Activity Assays: Rac activity is determined from lysates of the MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines (from ATCC). 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. |
细胞实验 | MDA-MB-231, MDA-MB-435, or MCF-10A mammary epithelial cells (from ATCC) are incubated in vehicle (0.1% DMSO) or varying concentrations of EHop-016 (0–10 μM) for 24 h. Cell viability is measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit according to the manufacturer's instructions.(Only for Reference) |
别名 | EHop 016 |
分子量 | 430.55 |
分子式 | C25H30N6O |
CAS No. | 1380432-32-5 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (116.13 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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