Fasudil (HA-1077) HCl

Catalog No.S1573 Synonyms: AT-877

For research use only.

Fasudil (HA-1077, AT-877), 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. Fasudil is also a calcium channel blocker.

Fasudil (HA-1077) HCl Chemical Structure

CAS No. 105628-07-7

Selleck's Fasudil (HA-1077) HCl has been cited by 73 publications

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Biological Activity

Description Fasudil (HA-1077, AT-877), 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. Fasudil is also a calcium channel blocker.
Rho [1] Calcium channel [2] ROCK2 [1]
(Cell-free assay)
PKA [1]
(Cell-free assay)
PKG [1]
(Cell-free assay)
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330 nM(Ki) 1.6 μM(Ki) 1.6 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
U937 cells MYXGeY5kfGmxbjDhd5NigQ>? MofFTY5pcWKrdHnvckBw\iCPQ2CxMYlv\HWlZXSgZ4hmdW:2YYjpd{BqdiCXOUO3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEOFUkKsJGlEPTB;M{Wg{txONg>? NFvLeYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{C4OFA5Pyd-MUewPFQxQDd:L3G+
Sf9 cells NVHWOZdqTnWwY4Tpc44h[XO|YYm= NXX4bJA2UW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJIh2dWGwIF3TT|Eh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD13IN88UU4> MnT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB7OUizOVEoRjFyOUm4N|UyRC:jPh?=
HEK293 cells MlTDSpVv[3Srb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKEircz30ZYdo\WRiaIXtZY4hWFKNMjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|LDDJR|UxRTRizszNMi=> M4nHeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyOUm4N|UyLz5zMEm5PFM2OTxxYU6=
Sf9 cells NUi3SW1bTnWwY4Tpc44h[XO|YYm= NFzwUZRKdmirYnn0bY9vKG:oIILheEBTV0ONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVEvQSEQvF2u MnHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB7OUizOVEoRjFyOUm4N|UyRC:jPh?=
insect cells M1PlVmZ2dmO2aX;uJIF{e2G7 M13vXlExKG2rboO= M2fRXGlvcGmkaYTpc44hd2ZiaIXtZY4hdGW3a3;jfZRq[yCUT1PLNUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJJV{cW6pIFvLVm5TXEyVVjDhd{B{fWK|dILheIUh[W[2ZYKgNVAhdWmwczDifUBxgXK3dnH0[UBscW6jc3WvcIFkfGG2ZTDk[Yh6\HKxZ3XuZZNmKGOxdYDs[YQh[XO|YYmsJGtqRTBwNUOg{txONg>? NGXHcnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkCzPVU4OCd-Mk[wN|k2PzB:L3G+
Sf9 cells NXHufIJmTnWwY4Tpc44h[XO|YYm= M3fpdVkxKG2rboO= NU\XVmFIUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rbnHsJIhqey22YXfn[YQhWk:FS{GgLFMuPTR|KTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JINmdGy|IIXzbY5oKEKrb4Tpck1CcHhvQVvSVmxUW0yUQT3DU25JOiC|dXLzeJJifGViYX7kJHto[W2vYT2zN3BeSVSSIHHmeIVzKDlyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBxem:6aX3peJkh[XO|YYmsJGlEPTB;MD6zJO69VS5? NFHiS2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{CxPFY6Oyd-MUewNVg3QTN:L3G+
A673 NELjVYxyUFSVIHHzd4F6 MlHjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MoXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Methods Test Index PMID
Western blot ROCK2 / p-ROCK2 / MLC2 / p-MLC2 ; ABCG2 ; Moesin / p-Moesin / β-catenin / p-β-catenin 29416017
Immunofluorescence p-ROCK2 / ABCG2 29416017
Growth inhibition assay Cell viability 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 (from reference)

Solubility (25°C)

In vitro

In vivo

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(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 327.83


CAS No. 105628-07-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl

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