产品说明书
EHT 1864
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同义名 : | EHT 1864 2HCl |
| CAS号 : | 754240-09-0 | |
| 货号 : | A638191 | |
| 分子式 : | C25H29Cl2F3N2O4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 581.475 | |
| MDL号 : | MFCD11114384 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(51.59 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 100 mg/mL(171.98 mM) |
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| 动物实验配方： |
| 生物活性 | |||
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| 靶点 |
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| 描述 | Rho family proteins (20 human members) comprise a major branch of the Ras superfamily of small GTPases. Like Ras, Rho GTPases function as GDP/GTP-regulated binary on-off switches. Rho GTPases are regulators of a diverse variety of cellular processes that include regulation of cell proliferation, actin cytoskeleton reorganization, and gene expression. EHT 1864, a small molecule inhibitor, which attenuates Rac1 activation by retaining the G-protein in an inert/inactive state, thereby preventing activation of its downstream effector proteins. EHT 1864 possesses high affinity binding to Rac1, as well as the related Rac1b, Rac2, and Rac3 isoforms with KD of 40 nM, 50 nM, 60 nM and 250 nM, respectively. EHT 1864 can inhibit a variety of downstream signaling activities activated by ectopic expression of constitutively-activated Rac1(G12V) and decreased Rac1 association with the isolated Rho GTPase binding domain (RBD) of the p21-activated serine/threonine kinase effector PAK1in vivo. NIH 3T3 cells were incubated for 16 h in serum-free growth medium, either alone, or supplemented with 5 μM EHT 1864 for the last 4 h. It was found that EHT 1864-treated cells showed an ∼80% reduction in PDGF stimulation of lamellipodia which demonstrated that EHT 1864 is a potent and specific inhibitor of PDGF-induced lamellipodia formation[3]. In vitro study, after pre-incubation at varying concentrations of EHT 1864 (0–10 μM) for 1 h, INS-1 832/13 cells were further incubated in the presence of low (2.5 mM) or varying concentrations of glucose (2.5-20 mM) or KCl (40 mM) for 30 min at 37 °C, the result showed that EHT 1864 inhibited glucose-induced Rac1 activation in INS-1 832/13 cells, which resulted in inhibition of GSIS (Glucose-stimulated insulin secretion)[4]. C57BL/6 mice were injected EHT-1864 once a day for 7 days. It was determined that EHT-1864 efficiently inhibits the expression of Rac1, Rac2, and Rac3. And colon length was observed recovered after EHT-1864 treatment for 5 days. Furthermore, less inflammation-associated rectal bleeding and soft stool were observed in the EHT-1864 treatment group, which demonstrate the preventive role of EHT-1864 on acute colitis in mice[5]. | ||
| 作用机制 | EHT 1864 binds to Rac1 with high affinity, and retains Rac1 in an inert and inactive state by displacement of pre-bound guanine nucleotide (GDP/GTP). | ||
| 细胞研究 | |||||
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| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| 293T cells | Function assay | Effect on Rac1 binding to RhoGDI2 expressed in 293T cells by Western blot analysis | 17932039 | ||
| mouse NIH3T3 cells | Function assay | Effect on Rac1 binding to RhoGDI2 in mouse NIH3T3 cells by Western blot analysis | 17932039 | ||
| mouse NIH3T3 cells | Function assay | Effect on Rac1 binding to RhoGDI1 in mouse NIH3T3 cells by Western blot analysis | 17932039 | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.72mL 0.34mL 0.17mL |
8.60mL 1.72mL 0.86mL |
17.20mL 3.44mL 1.72mL |
| 参考文献 |
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