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

Fasudil (Synonyms: HA-1077; AT877)

Cat. No.: HY-10341A
Handling Instructions

Fasudil (HA-1077; AT877), is a nonspecific 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.

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 MCE. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364.

    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 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[1]. Fasudil is also a potent Ca2+channel antagonist and vasodilator[2].

    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 and human HSC-derived TWNT-4 cells[4].
    Fasudil (50-100 μM; 24 hours) inhibits the LPA-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].

    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 (intravenous injection; 0.01, 0.03, 0.1 and 0.3 mg/kg) decreases MBP and increases HR, VBF, CBF, RBF, and FBF.
    Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via 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 obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs[5].
    Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[6].
    Fasudil (orally administration; 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration[7].

    Clinical Trial
    Molecular Weight

    291.37

    Formula

    C₁₄H₁₇N₃O₂S

    CAS No.

    103745-39-7

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage

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

    References
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