Fasudil (HA-1077) HCl

Catalog No.S1573

Fasudil (HA-1077) HCl Chemical Structure

Molecular Weight(MW): 327.83

Fasudil(HA-1077), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively.

Size Price Stock Quantity  
In DMSO USD 88 In stock
USD 97 In stock
USD 170 In stock
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Cited by 36 Publications

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Biological Activity

Description Fasudil(HA-1077), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively.
Targets
ROCK2 [1]
(Cell-free assay)
PKA [1]
(Cell-free assay)
PKG [1]
(Cell-free assay)
PKC [1]
(Cell-free assay)
330 nM(Ki) 1.6 μM(Ki) 1.6 μM(Ki) 3.3 μM(Ki)
In vitro

Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. [2] Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. [3] Fasudil induces disorganization of actin stress fiber and cell migration inhibition. [4] Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 cells M1P1NmZ2dmO2aX;uJIF{e2G7 NH7XZ4I6OCCvaX7z MojyTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCQLYTldo1qdmGuIHjpd{11[WepZXSgVm9EUzFiKEOtOVQ{MSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHPlcIx{KHW|aX7nJGJqd3Srbj3BbJguSUuUUlzTV2xTSS2FT17INkB{fWK|dILheIUh[W6mIGvnZY1u[S1|M2DdRXRRKGGodHXyJFkxKG2rboOgZpkhe2OrboTpcIxifGmxbjDwdo95cW2rdImgZZN{[XluIFnDOVA:OC5|IN88UU4> MkPRNVcxOTh4OUO=
insect cells Mk\GSpVv[3Srb36gZZN{[Xl? M4L2Z|ExKG2rboO= M1L6TmlvcGmkaYTpc44hd2ZiaIXtZY4hdGW3a3;jfZRq[yCUT1PLNUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJJV{cW6pIFvLVm5TXEyVVjDhd{B{fWK|dILheIUh[W[2ZYKgNVAhdWmwczDifUBxgXK3dnH0[UBscW6jc3WvcIFkfGG2ZTDk[Yh6\HKxZ3XuZZNmKGOxdYDs[YQh[XO|YYmsJGtqRTBwNUOg{txONg>? M4OyelI3ODN7NUew
Sf9 cells NV3xd5FKTnWwY4Tpc44h[XO|YYm= NGLacXJKdmirYnn0bY9vKG:oIILheEBTV0ONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVEvQSEQvF2u NXL4b3Y4OTB7OUizOVE>
HEK293 cells NHqwPXlHfW6ldHnvckBie3OjeR?= NHTONVRKdmirYnn0bY9vKG:oIFjpd{11[WepZXSgbJVu[W5iUGLLNkBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzMEBKSzVyPUSg{txONg>? MYWxNFk6QDN3MR?=
Sf9 cells M1HlNGZ2dmO2aX;uJIF{e2G7 NH;Me49KdmirYnn0bY9vKG:oIFjpd{11[WepZXSgbJVu[W5iTWPLNUBmgHC{ZYPz[YQhcW5iU3[5JINmdGy|LDDJR|UxRTVizszNMi=> NYj2UYVPOTB7OUizOVE>
U937 cells M3iydmZ2dmO2aX;uJIF{e2G7 NH;0V3hKdmirYnn0bY9vKG:oIF3DVFEucW6mdXPl[EBkcGWvb4ThfIl{KGmwIGW5N|ch[2WubIOgc5ZmemW6cILld5NqdmdiQ1PSNkwhUUN3ME2zOUDPxE1w MX[xO|A5PDB6Nx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ROCK2 / p-ROCK2 / MLC2 / p-MLC2 ; 

PubMed: 29416017     


Expression of ROCK2, p-ROCK2, MLC2 and p-MLC2 was determined under stimulation of fasudil (0.4, 2, 10 μM). 

ABCG2; 

PubMed: 29416017     


All resistant cells were treated with fasudil (0.4, 2, 10 μM) for 24 h, and total, membrane (M) and cytoplasm (c) expression of ABCG2 was examined by western blot.

Moesin / p-Moesin / β-catenin / p-β-catenin ; 

PubMed: 29416017     


U251R and rG-1 were stimulated by fasudil (0.4, 2, 10 μM) for 24 h, and protein levels of ROCK2, p-ROCK2, moesin, p-moesin (Thr 558), β-catenin, p-β-catenin (Ser 552) were detected by western blot. β-Catenin expressions of nucleus (N) and cytoplasm (C) were detected.

29416017
Immunofluorescence
p-ROCK2 / ABCG2 ; 

PubMed: 29416017     


f, g U251R (g) and rG-1 (f) were stimulated with fasudil (10 μM), IF was used to analyze expression of p-ROCK2 and ABCG2 (p-ROCK2: red, ABCG2: green; scale bar, 20 μm). GAPDH and flotillin-1 were used as loading control. Statistical differences compared with the control 

29416017
Growth inhibition assay
Cell viability; 

PubMed: 29262624     


MTT was used to determine the IC50 of FSD in HUVEC cells cultured in standard condition. 

29262624
In vivo Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. [3] Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. [6] The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice. [7]

Protocol

Solubility (25°C)

In vitro Water 65 mg/mL (198.27 mM)
DMSO 5 mg/mL (15.25 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 327.83
Formula

C14H17N3O2S.HCl

CAS No. 105628-07-7
Storage powder
in solvent
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID