Fasudil (HA-1077) HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Fasudil (HA-1077) HCl是一种选择性的ROCK抑制剂, IC50值为0.74μM[1]。
Rho-相关蛋白激酶(ROCK)属于丝氨酸-苏氨酸激酶AGC家族, 其在调节多种细胞进程中发挥关键作用。据报道, ROCK的异常表达与许多疾病和传染病有关[2]。
Fasudil (HA-1077) HCl是有效的ROCK抑制剂,它与已报道的抑制剂Y-27632有着不同的结构。在两个人膀胱癌细胞系(5637和UM-UC-3)中, Fasudil (HA-1077) HCl通过阻断Rho/ROCK通路,以剂量依赖的方式抑制细胞增殖,减少细胞迁移并诱导细胞凋亡[3]。在口腔鳞状细胞癌SCC-4细胞中,Fasudil (HA-1077) HCl可显著降低细胞运动,并以剂量依赖的方式抑制细胞迁移和侵袭(1,50和 100 μmol/L)[4]。
在由缺陷引发的骨髓增殖性疾病Cbl/Cbl-b小鼠模型中,Fasudil (HA-1077) HCl(100 毫克/千克,每日)口服给药可明显提高白细胞总数和单核细胞数,延长生存时间,但与对照组相比无统计差异[2]。
参考文献:
1]. Wickman, G., C. Lan, and B. Vollrath, Functional roles of the rho/rho kinase pathway and protein kinase C in the regulation of cerebrovascular constriction mediated by hemoglobin: relevance to subarachnoid hemorrhage and vasospasm. Circ Res, 2003. 92(7): p. 809-16.
[2]. William, B.M., et al., Fasudil, a clinically safe ROCK inhibitor, decreases disease burden in a Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders. Hematology, 2015.
[3]. Abe, H., et al., The Rho-kinase inhibitor HA-1077 suppresses proliferation/migration and induces apoptosis of urothelial cancer cells. BMC Cancer, 2014. 14: p. 412.
[4]. Moreira Carboni, S.S., et al., HA-1077 inhibits cell migration/invasion of oral squamous cell carcinoma. Anticancer Drugs, 2015.
2. Hu, Haiyan, et al. "Fasudil prevents calcium oxalate crystal deposit and renal fibrogenesis in glycoxylate-induced nephrolithic mice." Experimental and Molecular Pathology (2015). PMID:25697583
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 327.83 |
Cas No. | 105628-07-7 |
Formula | C14H17N3O2S·HCl |
Solubility | ≥16.4 mg/mL in DMSO; ≥4.81 mg/mL in EtOH with ultrasonic; ≥50 mg/mL in H2O |
Chemical Name | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride |
SDF | Download SDF |
Canonical SMILES | C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
5637, UM-UC-3 以及 SCC-4细胞系 |
溶解方法 |
在DMSO中的溶解度> 16.4 mg/ml。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
0~30μM |
应用 |
Lysophosphatidic acid和geranylgeraniol可以引起细胞增殖和迁移的增加,该效应与RhoA活性的升高以及ROCK表达的上调有关。Fasudil(HA-1077)可以有效地抑制细胞增殖和迁移,并以剂量依赖的方式诱导细胞凋亡。 此外,Fasudil(HA-1077)也可以显著抑制ROCK-I和ROCK-II的表达,但不影响RhoA活性。 |
动物实验 [2]: | |
动物模型 |
Cbl/Cbl-b缺陷驱动的鼠骨髓增生性疾病模型 |
剂量 |
100 mg/kg /天,口服 |
应用 |
在Cbl/Cbl-b缺陷驱动的鼠骨髓增生性疾病模型中,通过2周的治疗,用fasudil治疗的小鼠中,总白细胞和单核细胞计数显著降低。 同时,还观察到fasudil治疗小鼠存活率提高的趋势,但并未达到统计学差异。 值得注意的是,在两个fasudil治疗的小鼠中,研究观察到超过27周的长期存活率,两倍于Cbl / Cbl-b DKO MPD模型中16周平均寿命。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Abe, H., et al., The Rho-kinase inhibitor HA-1077 suppresses proliferation/migration and induces apoptosis of urothelial cancer cells. BMC Cancer, 2014. 14: p. 412. [2] William, B.M., et al., Fasudil, a clinically safe ROCK inhibitor, decreases disease burden in a Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders. Hematology, 2015. |
质量控制和MSDS
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