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HA-1077

Fasudil, Eril, AT-877

A Rho/Rok Inhibitor

Cat #: H-220
Alternative Name Fasudil, Eril, AT-877
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 364.3
    Purity: >99%
    Effective concentration >1 µM.
    Structure
    Chemical name 1-(5-Isoquinolinesulfonyl) homopiperazine, dihydrochloride salt.
    Molecular formula C14H17N3O2S•2HCl.
    CAS No.: 103745-39-7
    Activity HA-1077 specifically inhibits the small GTPase – Rho through its associated kinase-Rho dependent kinase (ROK), thereby inhibiting myosin llight chain (MLC) phosphorylation1-3. It also acts as an intracellular Ca2+ antagonist4.
    References-Activity
    1. Asano, T. et al. (1989) Br. J. Pharmacol98, 1091.
    2. Uehata, M. et al. (1997) Nature 389, 990.
    3. Nagumo, H. et al.(2000) Am. J. Physiol278, C57.
    4. Takayasu, M. et al. (1989) J. Neurosurg65, 80.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Water, DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Our bioassay
    • Alomone Labs HA-1077 inhibits the phosphorylation of myosin light chain (MLC) in C2C12 cells.
      Alomone Labs HA-1077 inhibits the phosphorylation of myosin light chain (MLC) in C2C12 cells.
      Cells were grown in fetal calf serum (FCS) to 2 days post-confluence. They were then stimulated with 2% horse serum (HS) or not (FCS) in the presence or absence of 20 µM HA-1077 (#H-220) for the indicated times. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho- MLC.
    References - Scientific background
    1. Asano, T. et al. (1989) Br. J. Pharmacol98, 1091.
    2. Uehata, M. et al. (1997) Nature 389, 990.
    3. Nagumo, H. et al.(2000) Am. J. Physiol. Cell Physiol. 278, C57.
    4. Shirotani, M. et al. (1991) J. Pharmacol. Exp. Ther. 259, 738.
    5. Sasaki, Y. et al. (1987) Am. J. Physiol253, C71.
    6. Seto, M. et al. (1991) Eur. J. Pharmacol195, 267.
    7. Asano, T. et al. (1987) J. Pharmacol. Exp. Ther241, 1033.
    8. Takayasu, M. et al. (1986)  J. Neurosurg65, 80.
    9. Takizawa, S. et al. (1993) Eur. J. Pharmacol250, 431.
    Scientific background

    HA-1077 is a small, cell permeable derivative of isoquinoline which specifically inhibits the small GTPase - Rho by inhibition of its associated kinase-Rho dependent kinase (ROK). This signaling pathway acts as a molecular switch to control cytoskeleton organization in many cell types including smooth muscle.1-3 By inhibition of ROK, HA-1077 decreases the myosin light chain (MLC) phosphorylation induced by Ca2+ due to abrogating Rho-mediated inhibition of MLC dephosphorylation. HA-1077 also inhibits fetal calf serum-induced proliferation and [3H]thymidine incorporation into DNA of growth-arrested VSMC in a dose-dependent manner.4-6

    At concentrations higher than 5 µM, it induces disorganization of actin filament structure. This compound was also found to act as a vasodilator and antivasospasm drug which antagonizes the verapamil-insensitive voltage dependent Ca2+ channel and is used clinically for treatment of the cerebral vasospasm after subarachnoid hemorrhage.7-9

    Last update: 11/04/2021

    HA-1077 (#H-220) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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