EHT 1864
目录号 : GC10660
An inhibitor of Rac GTPases
Cas No.:754240-09-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
INS-1 832/13 cells (Insulin-Producing-Cell Line) |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
1 h |
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Applications |
10 μM EHT 1864 shows a complete inhibition of GSIS (Glucose-stimulated insulin secretion)and inhibits GSIS at 10-20mM glucose. It also suppresses a glucose-induced membrane association of Rac1 and glucose-induced ERK1/2 phosphorylation and activation. |
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References: 1. Sidarala V, Veluthakal R, Syeda K, Kowluru A. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells. Cell Signal. 2015 Jun;27(6):1159-67. | |
EHT 1864 is a small-molecule inhibitor of Rac family small GTPases with Kd value of 40nM for Rac1 [1].
In NIH 3T3 mouse fibroblasts, EHT 1864 treatment shows an 80% reduction in PDGF-induced lamellipodia formation. EHT 1864 at concentration of 50μM can completely inhibit the complex formation between Rac1 and PAK-RBD and cause the release of nucleotide from Rac1. The reassociation of nucleotide with Rac1 induced by EDTA or the Tiam1 can also be blocked by EHT 1864. EHT 1864 is most potent to Rac1, both in the binding affinity and stimulation of nucleotide release. It binds to Rac1b, Rac2 and Rac3 with Kd values of 50nM, 60nM and 250nM, respectively. Moreover, EHT 1864 can suppress cellular transformation induced by Rac1 with an 80% inhibition of focus-forming activity [1].
References:
[1] Shutes A, Onesto C, Picard V, et al. Specificity and mechanism of action of EHT 1864, a novel small molecule inhibitor of Rac family small GTPases. Journal of Biological Chemistry, 2007, 282(49): 35666-35678.
| Cas No. | 754240-09-0 | SDF | |
| Canonical SMILES | FC(F)(C1=CC=C2C(SCCCCCOC3=COC(CN4CCOCC4)=CC3=O)=CC=NC2=C1)F.Cl.Cl | ||
| 分子式 | C25H29Cl2F3N2O4S | 分子量 | 581.48 |
| 溶解度 | ≥ 29.05mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7197 mL | 8.5987 mL | 17.1975 mL |
| 5 mM | 0.3439 mL | 1.7197 mL | 3.4395 mL |
| 10 mM | 0.172 mL | 0.8599 mL | 1.7197 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。