1. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton Neuronal Signaling Membrane Transporter/Ion Channel Autophagy Epigenetics
  2. ROCK Calcium Channel Autophagy PKA PKC
  3. 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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Fasudil Hydrochloride) that retains the same biological activity.

For research use only. We do not sell to patients.

Fasudil Chemical Structure

Fasudil Chemical Structure

CAS No. : 103745-39-7

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Top Publications Citing Use of Products

    Fasudil purchased from MedChemExpress. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364.  [Abstract]

    RhoA and ROCK2 upregulation in the rat hippocampus is involved in memory dysfunction induced by postnatal exposure of Sevoflurane. The expression of RhoA, ROCK2 and cleaved caspase-3 (Cl-Csp3) in the hippocampus of the S3 group significantly increased, compared to that of the C group (P<0.05). There is no difference of the level of RhoA, ROCK2 and Cl-Csp3 between the C and S1 groups (P>0.05). ROCK2 inhibitor Fasudil hydrochloride in the F group clearly decreases the expression of ROCK2 and Cl-Cs

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    Description

    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].

    IC50 & Target[1]

    p160ROCK

    0.33 μM (Ki)

    ROCK2

    0.158 μM (IC50)

    PKA

    4.58 μM (IC50)

    PKC

    12.3 μM (IC50)

    PKG

    1.65 μM (IC50)

    In Vitro

    Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells[4].
    Fasudil (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells[4].
    Fasudil (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[4]

    Cell Line: Rat HSCs and human HSC-derived TWNT-4 cells
    Concentration: 50 μM; 100 μM
    Incubation Time: 24 hours
    Result: Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.

    RT-PCR[4]

    Cell Line: Rat HSCs and human HSC-derived TWNT-4 cells
    Concentration: 25 μM; 50 μM; 100 μM
    Incubation Time: 24 hours
    Result: Reduced the expression of type I collagen, a-SMA, and TIMP-1.
    In Vivo

    Fasudil (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[5].
    Fasudil (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio[6].
    Fasudil (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice[6].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Myocardial ischemia and reperfusion in rat (250-300 g)[5]
    Dosage: 10 mg/kg
    Administration: Intravenous injection; 1 h before operation
    Result: Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus.
    Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.
    Clinical Trial
    Molecular Weight

    291.37

    Formula

    C14H17N3O2S

    CAS No.
    SMILES

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

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    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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