Fasudil

Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+ channel antagonist and vasodilator[1][2][3].

Product Specifications

CAS Number

[103745-39-7]

Product Name Alternative

HA-1077; AT877

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Autophagy; Calcium Channel; PKA; PKC; ROCK

Type

Reference compound

Related Pathways

Autophagy; Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; Membrane Transporter/Ion Channel; Neuronal Signaling; Stem Cell/Wnt; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/fasudil.html

Purity

99.91

Solubility

DMSO : 33.33 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O

Molecular Formula

C14H17N3O2S

Molecular Weight

291.37

Precautions

H302, H315, H319, H335

References & Citations

[1]Chen M, et al. Fasudil and its analogs: a new powerful weapon in the long war against central nervous system disorders? Expert Opin Investig Drugs. 2013 Apr;22 (4) :537-50.|[2]Huang XN, et al. The effects of fasudil on the permeability of the rat blood-brain barrier and blood-spinal cordbarrier following experimental autoimmune encephalomyelitis. J Neuroimmunol. 2011 Oct 28;239 (1-2) :61-7.|[3]Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389 (6654) :990-4.|[4]Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25 (4) :829-38.|[5]Zhang J, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia/reperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401 (1-2) :76-80.|[6]Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180 (1-2) :126-34. Epub 2006 Sep 22.