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Fasudil (HA-1077) HCl

カタログ番号GC14289

Fasudil(HA-1077; AT877)塩酸塩は非特異的RHOA/ROCK阻害剤であり、0.33 &#############788787878788788788878878887###8年にかうしたタンパク質キナーゼにも阻害効果があります。 offlineefficient_models_2022q2.md;M, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively.en_ja_2022q2.mdFasudil (HA-1077) HCl is also a potent Ca2+ channel antagonist and vasodilator.en_ja_2022q2.md

Products are for research use only. Not for human use. We do not sell to patients.

Fasudil (HA-1077) HCl 化学構造

Cas No.: 105628-07-7

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$39.00
在庫あり
200mg
$52.00
在庫あり
500mg
$93.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

5637, UM-UC-3 and SCC-4 cell lines

Preparation method

The solubility of this compound in DMSO is >16.4 mg/ml. 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.

Reacting condition

0-30 μM

Applications

Lysophosphatidic acid and geranylgeraniol induced an increase of cell proliferation and migration in association with promotion of RhoA activity and upregulation of ROCK expression. Fasudil (HA-1077) could suppress cell proliferation and migration, and also induce apoptosis in a dose-dependent manner. Fasudil (HA-1077) also dramatically suppressed the expression of ROCK-I and ROCK-II, but did not affect RhoA activity.

Animal experiment [2]:

Animal models

Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders

Dosage form

100 mg/kg daily by oral gavage

Application

In the Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders, by 2 weeks of treatment, total white cell and monocyte counts were significantly lower in mice treated with fasudil. A trend towards improved survival in fasudil-treated mice that did not reach statistical significance was also observed. Notably, prolonged survival beyond 27 weeks was seen in two fasudil-treated mice, nearly twice the 16-week average life-span in the Cbl/Cbl-b DKO MPD model.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

Background

Fasudil (HA-1077) HCl is a selective inhibitor of ROCK with IC50 value of 0.74 μM [1].

Rho-associated protein kinase (ROCK) belongs to the AGC family of serine-threonine kinases and plays a pivotal role in regulating a variety of cellular processes. It has been reported that abnormal expression of ROCK is correlated with numerous diseases and infections [2].

Fasudil (HA-1077) HCl is a potent ROCK inhibitor and has a different structure with the reported ROCK inhibitor Y-27632. When tested with 2 human bladder cancer cell lines (5637 and UM-UC-3), Fasudil (HA-1077) HCl treatment inhibits cell proliferation, decreases cell migration and induced cell apoptosis in a dose dependent manner via blocking Rho/ROCK pathway [3]. In oral squmous cell carcinoma SCC-4 cells, administration of Fasudil (HA-1077) HCl markedly decreases cell motility and inhibits cell migration or invasion in a dose dependent manner (1, 50 and 100 μmol/L [4].

In the Cbl/Cbl-b deficiency-driven murine model of myeloproliferative disorders, oral administration of Fasudil (HA-1077) HCl (100 mg/kg, daily) markedly increases the total white cell and monocyte numbers while prolonged survival time has trend but no statistical difference compared with the control group [2].

References:
[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.

Chemical Properties

Cas No. 105628-07-7 SDF
Chemical Name 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride
Canonical SMILES C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
Formula C14H17N3O2S.HCl M.Wt 327.83
溶解度 ≥ 16.4mg/mL in DMSO, ≥ 4.81 mg/mL in EtOH with ultrasonic, ≥ 50 mg/mL in Water Storage Store at 4°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.0504 mL 15.2518 mL 30.5036 mL
5 mM 0.6101 mL 3.0504 mL 6.1007 mL
10 mM 0.305 mL 1.5252 mL 3.0504 mL
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Review for Fasudil (HA-1077) HCl

Average Rating: 5 ★★★★★ (Based on Reviews and 14 reference(s) in Google Scholar.)

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