ROCK inhibitor-2
目录号 : GC37551
ROCK inhibitor-2是一种选择性Rho激酶（ROCK）抑制剂，抑制ROCK1和ROCK2的IC50值分别为17nM和2nM，具有抗肿瘤活性。
Cas No.:1127308-52-4
Sample solution is provided at 25 µL, 10mM.
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ROCK inhibitor-2 is a selective Rho kinase (ROCK) inhibitor with IC50 values of 17nM and 2nM for ROCK1 and ROCK2, respectively, and has anti-tumor activity[1, 2]. ROCK is a serine/threonine protein kinase and a downstream target effector molecule of Rho. ROCK can regulate multiple functions such as cell contraction, migration, adhesion and proliferation[3, 4]. ROCK inhibitor-2 belongs to the aminopyridine class of compounds and is a structural analog of Y-27632[5]. ROCK inhibitor-2 may help improve vision loss and treat glaucoma[6].
In vitro, treatment of human osteosarcoma cell line (U2OS cells) with ROCK inhibitor-2 (50μM) for 48h significantly inhibited cell migration and invasion and caused mitochondrial dysfunction[2].
References:
[1]Feng Y, LoGrasso P V, Defert O, et al. Rho kinase (ROCK) inhibitors and their therapeutic potential[J]. Journal of medicinal chemistry, 2016, 59(6): 2269-2300.
[1] Zhang W, Zhao W, Li Q, et al. 3D-printing magnesium–polycaprolactone loaded with melatonin inhibits the development of osteosarcoma by regulating cell-in-cell structures[J]. Journal of Nanobiotechnology, 2021, 19: 1-20.
[3]Liu J, Wada Y, Katsura M, et al. Rho-associated coiled-coil kinase (ROCK) in molecular regulation of angiogenesis[J]. Theranostics, 2018, 8(21): 6053.
[4]Liao J K, Seto M, Noma K. Rho kinase (ROCK) inhibitors[J]. Journal of cardiovascular pharmacology, 2007, 50(1): 17-24.
[5]Shahin R, Shaheen O, El-Dahiyat F, et al. Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment[J]. Future science OA, 2017, 3(4): FSO204.
[6]Abbhi V, Piplani P. Rho-kinase (ROCK) inhibitors-a neuroprotective therapeutic paradigm with a focus on ocular utility[J]. Current Medicinal Chemistry, 2020, 27(14): 2222-2256.
ROCK inhibitor-2是一种选择性Rho激酶（ROCK）抑制剂，抑制ROCK1和ROCK2的IC50值分别为17nM和2nM，具有抗肿瘤活性[1, 2]。ROCK是丝氨酸/苏氨酸蛋白激酶，属于Rho下游靶效应分子，能够调节细胞收缩、迁移、黏附和增殖等多种功能[3, 4]。ROCK inhibitor-2属于氨基吡啶类化合物，是Y-27632的结构类似物[5]。ROCK inhibitor-2可能有助于改善视力丧失，治疗青光眼[6]。
在体外，ROCK inhibitor-2（50μM）处理人骨肉瘤细胞系（U2OS细胞）48h，显著抑制了细胞迁移和侵袭，并导致线粒体功能障碍[2]。
| Cell experiment [1]: | |
Cell lines | U2OS cells |
Preparation Method | U2OS cells were seeded in 6-well plates at a density of 8.5×105/well, and 1mM melatonin and 50µM ROCK inhibitor-2 were added. After 48h of culture, the cells were scratched with a pipette tip. Subsequently, they were incubated with DMEM medium containing 0.5% FBS. After repeated treatment at 0, 12, 24, and 48h, cell photos were taken using a phase contrast microscope. |
Reaction Conditions | 50μM; 48h |
Applications | ROCK inhibitor-2 treatment significantly reduced the cell migration area. |
References: | |
| Cas No. | 1127308-52-4 | SDF | |
| Canonical SMILES | O=C(N[C@H](C)C1=CC=CC(OC)=C1)C(C=C2)=CC=C2C3=CC=NC=C3 | ||
| 分子式 | C21H20N2O2 | 分子量 | 332.4 |
| 溶解度 | DMSO: 250 mg/mL (752.11 mM) | 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 | 3.0084 mL | 15.0421 mL | 30.0842 mL |
| 5 mM | 0.6017 mL | 3.0084 mL | 6.0168 mL |
| 10 mM | 0.3008 mL | 1.5042 mL | 3.0084 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 | ||||||||||
| 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，
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2.
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Quality Control & SDS
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- Purity: >98.00%
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