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

ROCK1 Inhibitor

ROCK1 Inhibitors (45):

Cat. No. Product Name Effect Purity
  • HY-10071
    Y-27632
    		Inhibitor 99.91%
    Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
  • 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 99.42%
    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 99.96%
    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-168650
    ROCK/HDAC-IN-1
    		Inhibitor
    ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity.
  • HY-16758A
    Verosudil hydrochloride
    		Inhibitor
    Verosudil hydrochloride (AR-12286 hydrochloride) is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is an inhibitor for Rho-kinase (ROCK) with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. Verosudil hydrochloride lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork.
  • HY-162596
    NRL-1049
    		Inhibitor
    NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice.
  • HY-15556
    GSK269962A
    		Inhibitor 99.83%
    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-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-11000
    GSK429286A
    		Inhibitor 98.17%
    GSK429286A is a selective inhibitor of ROCK1 with an IC50 value of 14 nM.
  • 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.
  • HY-16071
    AT13148
    		Inhibitor 99.21%
    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-15755
    RKI-1447
    		Inhibitor 98.29%
    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-18990
    GSK180736A
    		Inhibitor 98.01%
    GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  • HY-15687A
    SAR407899
    		Inhibitor 99.60%
    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-10319
    BAY-549
    		Inhibitor 99.46%
    BAY-549 (Azaindole 1) 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-13911
    Hydroxyfasudil
    		Inhibitor 98.78%
    Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
  • 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.