EHop-016
目录号 : GC10030
EHop-016是一种高效的Rac GTP酶Rac1抑制剂，IC50值为1.1μM。
Cas No.:1380432-32-5
Sample solution is provided at 25 µL, 10mM.
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EHop-016 is a potent inhibitor of Rac GTPase Rac1, with an IC50 value of 1.1μM[1]. EHop-016 targets the Rac protein and reduces the activity of the downstream effector molecule, p21-activated kinase (PAK), thereby demonstrating cytotoxicity[2]. EHop-016 has been widely used as an anti-cancer agent, inhibiting tumor growth in both cell models and mouse models[3].
In vitro, EHop-016 treatment for 48 hours significantly inhibited the proliferation of Calu1, A549, and HOP62 cells, with IC50 values of 4.3, 9.12, and 4.8μM, respectively[4]. EHop-016 reduced the number of viable MOLM-13 cells with an EC50 of 11.3µM after 48h incubation[5]. Treatment with 5μM EHop-016 for 1 hour can inhibit the glucose-induced actin remodeling in INS-1 832/13 cells[6].
In vivo, EHop-016 treatment via intraperitoneal injection at a dose of 25mg/kg (three times a week) for 8 weeks significantly reduced tumor growth without causing weight changes in GFP-MDA-MB-435 cell-xenograft mice[7]. Administering a 30mg/kg dose of EHop-016 by intraperitoneal injection three times a week for 55 days led to a reduction in macrophage infiltration in the tumors of breast cancer mouse models, and decreased the activation of myeloid cells[8].
References:
[1] Montalvo-Ortiz B L, Castillo-Pichardo L, Hernández E, et al. Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase[J]. Journal of Biological Chemistry, 2012, 287(16): 13228-13238.
[2] Crespo G E V, Hernández E, Vlaar C, et al. The novel Rac inhibitor HV-107 as a potential therapeutic for metastatic breast cancer[J]. Cancer Research, 2018, 78(13_Supplement): 4185-4185.
[3] Asencio‐Torres G, Hernández E, Vlaar C, et al. Novel Rac Inhibitors as Targeted Therapeutics for Metastatic Breast Cancer[J]. The FASEB Journal, 2018, 32: 804.14-804.14.
[4] Yang J, Qiu Q, Qian X, et al. Long noncoding RNA LCAT1 functions as a ceRNA to regulate RAC1 function by sponging miR-4715-5p in lung cancer[J]. Molecular cancer, 2019, 18(1): 171.
[5] Hemsing A L, Førde J L, Reikvam H, et al. The Rac1-inhibitor EHop-016 attenuates AML cell migration and enhances the efficacy of daunorubicin in MOLM-13 transplanted zebrafish larvae[J]. Translational Oncology, 2024, 40: 101876.
[6] Veluthakal R, Tunduguru R, Arora D K, et al. VAV2, a guanine nucleotide exchange factor for Rac1, regulates glucose-stimulated insulin secretion in pancreatic beta cells[J]. Diabetologia, 2015, 58(11): 2573-2581.
[7] Castillo-Pichardo L, Humphries-Bickley T, De La Parra C, et al. The Rac inhibitor EHop-016 inhibits mammary tumor growth and metastasis in a nude mouse model[J]. Translational oncology, 2014, 7(5): 546-555.
[8] Torres-Sanchez A, Rivera-Robles M, Castillo-Pichardo L, et al. Rac and Cdc42 inhibitors reduce macrophage function in breast cancer preclinical models[J]. Frontiers in Oncology, 2023, 13: 1152458.
EHop-016是一种高效的Rac GTP酶Rac1抑制剂，IC50值为1.1μM[1]。EHop-016通过靶向Rac蛋白并降低下游效应分子p21激活激酶的活性，进而发挥细胞毒性作用[2]。EHop-016已作为抗癌剂广泛应用于细胞模型和小鼠模型中抑制肿瘤生长[3]。
在体外，EHop-016处理48小时能显著抑制Calu1、A549和HOP62细胞的增殖，IC50值分别为4.3μM、9.12μM和4.8μM[4]。经EHop-016处理48小时后，MOLM-13活细胞数量减少，EC50值为11.3µM[5]。使用5μM的EHop-016处理INS-1 832/13细胞1小时，可抑制葡萄糖诱导的肌动蛋白重构[6]。
在体内，每周三次腹腔注射25mg/kg剂量的EHop-016连续8周，能显著抑制GFP-MDA-MB-435细胞移植瘤小鼠的肿瘤生长，且未引起体重变化[7]。每周三次腹腔注射30mg/kg剂量的EHop-016连续55天，可减少乳腺癌小鼠模型肿瘤中的巨噬细胞浸润，并降低髓系细胞的活化水平[8]。
| Cell experiment [1]: | |
Cell lines | MDA-MB-435 cells |
Preparation Method | MDA-MB-435 cells were cultured in DMEM medium containing 10% fetal bovine serum (pH 7.5) at 37°C and 5% CO2. Cells were seeded in 96-well plates at a concentration of 2000 cells per well. EHop-016 was incubated in various concentrations (0, 0.1, 0.5, 1, 2, 4, 6, 8, and 10μM) for 24h, then MTT reagent was added, and absorbance was measured at 600nM. |
Reaction Conditions | 0, 0.1, 0.5, 1, 2, 4, 6, 8, and 10μM; 48h |
Applications | EHop-016 treatment significantly inhibited the viability of MDA-MB-435 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female nude mice |
Preparation Method | Female nude mice, aged 4 to 5 weeks, were housed in cages filtered by high-efficiency particulate air (HEPA) filters (5 mice per cage) and were maintained under pathogen-free (SPF) conditions. The lighting (12 hours of light/12 hours of darkness cycle), temperature (22 to 24°C), and humidity (25%) were all controlled. GFP-MDA-MB-435 cells (approximately 0.5×106 cells) were suspended in Matrigel and injected into the right fourth mammary fat pad of the mice under isoflurane inhalation (isoflurane concentration in the inhalation chamber was 1% to 3%, oxygen concentration was 2L/min) to establish an in situ primary tumor model. After tumor establishment (1 week after inoculation), mice from the same litter with similar body weight and tumor size were randomly divided into each experimental group. The mice received either the vehicle (12.5% ethanol, 12.5% Cremophor, and 75% 1×PBS pH 7.4) or 25mg/kg of EHop-016 by intraperitoneal injection three times a week for 8 weeks, and the tumor tissues were analyzed. |
Dosage form | 25mg/kg; three times a week for 8 weeks; i.p. |
Applications | EHop-016 treatment significantly reduced tumor growth without causing weight changes in GFP-MDA-MB-435 cell-xenograft mice. |
References: | |
| Cas No. | 1380432-32-5 | SDF | |
| 化学名 | 4-N-(9-ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine | ||
| Canonical SMILES | CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51 | ||
| 分子式 | C25H30N6O | 分子量 | 430.55 |
| 溶解度 | ≥ 25.6mg/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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3226 mL | 11.6131 mL | 23.2261 mL |
| 5 mM | 464.5 μL | 2.3226 mL | 4.6452 mL |
| 10 mM | 232.3 μL | 1.1613 mL | 2.3226 mL |
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| 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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，
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2.
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