1. Signaling Pathways
  2. Cell Cycle/DNA Damage
    Cytoskeleton
    Stem Cell/Wnt
    TGF-beta/Smad
  3. ROCK
  4. ROCK1 Isoform
  5. ROCK1 Inhibitor

ROCK1 Inhibitor

ROCK1 Inhibitors (57):

Cat. No. Product Name Effect Purity
  • HY-10071
    Y-27632
    Inhibitor 99.91%
    Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
  • HY-10583
    Y-27632 dihydrochloride
    Inhibitor 99.98%
    Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.
  • HY-15392
    Chroman 1
    Inhibitor 98.97%
    Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM.
  • HY-10341
    Fasudil Hydrochloride
    Inhibitor 99.97%
    Fasudil (HA-1077; AT877) Hydrochloride 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 Hydrochloride is also a potent Ca2+ channel antagonist and vasodilator.
  • HY-15307
    Belumosudil
    Inhibitor 99.83%
    Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
  • HY-181582
    LASSBio-2382
    Inhibitor
    LASSBio-2382 is a dual ROCK1/ROCK2 inhibitor with ROCK1 IC50 of 0.005 μM and ROCK2 IC50 of 0.003 μM. LASSBio-2382 inhibits viability and migration of cancer cells. LASSBio-2382 can be used for the research of triple-negative breast cancer.
  • HY-181583
    LASSBio-2389
    Inhibitor
    LASSBio-2389 is a selective ROCK2 inhibitor with an IC50 of 0.051 μM and an IC50 of 1.143 μM against ROCK1. LASSBio-2389 reduces the viability of MDA-MB-231 cells and inhibits cell migration. LASSBio-2389 is applicable to the research of triple-negative breast cancer.
  • HY-15556
    GSK269962A
    Inhibitor 99.75%
    GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities.
  • HY-11000
    GSK429286A
    Inhibitor 98.27%
    GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
  • HY-15685
    Ripasudil
    Inhibitor 99.95%
    Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
  • HY-10341A
    Fasudil
    Inhibitor 99.98%
    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.
  • HY-15307A
    Belumosudil mesylate
    Inhibitor 99.89%
    Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
  • HY-119937
    ROCK inhibitor-2
    Inhibitor 99.92%
    ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM. ROCK inhibitor-2 exhibits antitumor activity.
  • HY-15755
    RKI-1447
    Inhibitor 98.02%
    RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
  • HY-13300
    SR-3677
    Inhibitor 99.83%
    SR-3677 is a potent and selective ROCK-II inhibitor with an IC50 of ~3 nM.
  • HY-15687A
    SAR407899
    Inhibitor 99.67%
    SAR407899 is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
  • HY-16071
    AT13148
    Inhibitor 99.20%
    AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively.
  • HY-10319
    BAY-549
    Inhibitor 99.46%
    BAY-549 (Azaindole 1), a chemical probe, is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively.
  • HY-108518
    SB-772077B dihydrochloride
    Inhibitor 99.33%
    SB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases.
  • HY-13911A
    Hydroxyfasudil hydrochloride
    Inhibitor 98.88%
    Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.