EHT 1864
作者：齐岳
发布时间：2023-09-13
16:39:16
点击数：
产品名称：EHT 1864
产品描述：
| 产品描述 | EHT 1864 is a effective Rac family GTPase inhibitor for Rac1/Rac1b/Rac2/Rac3 (Kd: 40/50/60/250 nM). |
| 靶点活性 | Rac2:60 nM(Kd), Rac1b:50 nM(Kd), Rac3:250 nM(Kd), Rac1:40 nM(Kd) |
| 体外活性 | EHT 1864 selectively inhibits Rac-induced lamellipodia formation, and specifically reverses cell transformation induced by constitutively activated mutants of Rac1 and Tiam1. EHT 1864 strongly impaires oncogenic Ras-induced cell proliferation in NIH 3T3 cells stably expressing H-Ras(61L) protein. [1] EHT 1864 also reduces both extracellular and intracellular levels of Aβ peptides by inhibiting the γ-secretase-dependent cleavage of APP. [2] In cultured hippocampal pyramidal neurons, EHT 1864, via inhibition of Rac1, rescues the phenotype induced by Rich2 knock-down. [3] |
| 体内活性 | EHT 1864 (40 mg/kg i.p.) significantly reduces Abeta 40 and Abeta 42 levels in guinea pig brains. [2] |
| 激酶实验 | Inhibitor:GTPase binding analyses: For inhibitor:GTPase binding analyses, aliquots of small GTPase solution (containing 1 μM inhibitor) are titrated into a solution of 1 μM inhibitor in the cuvette. Changes in fluorescence anisotropy are monitored at λex = 360 nm, λem = 440 nm, 30 s after each addition. All data analysis and curve fitting were performed using Microsoft Excel and QuantumSoft's ProFit for Mac OS X. |
| 细胞实验 | NIH 3T3 cells stably expressing oncogenic Ras are plated in 96-well plates. The cells are cultured for up to 4 days in complete growth medium, either alone, or supplemented with 5 μM EHT 1864. Cell growth is then assessed using the conversion of MTT to a formazan product. Briefly, the MTT reagent (from a 5 mg/ml solution diluted in PBS) is added to the wells at a final concentration of 0.5 mg/ml, and the cells are further incubated for 4 h at 37°C. The medium is then removed, and the reaction is terminated by adding 100 μl/well Me2SO. The absorbance is read at 570 nm using a microplate reader.(Only for Reference) |
| 别名 | EHT 1864 2HCl |
| 分子量 | 581.47 |
| 分子式 | C25H29Cl2F3N2O4S |
| CAS No. | 754240-09-0 |
存储
| Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 43.6 mg/mL (75 mM)
H2O: 58.2 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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