2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Cytoskeleton
    Stem Cell/Wnt
    TGF-beta/Smad
  4. ROCK

ROCK

Rho-associated protein kinase; Rho-associated kinase; Rho-kinase; ROK

ROCK

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ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. ROCKs (ROCK1 and ROCK2) occur in mammals, zebrafish, Xenopus, invertebrates and chicken. Human ROCK1 has a molecular mass of 158 kDa and is a major downstream effector of the small GTPase RhoA. Mammalian ROCK consists of a kinase domain, acoiled-coil region and a Pleckstrin homology (PH) domain, which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular fold if RhoA-GTP is not present. ROCK plays a role in a wide range of different cellular phenomena, as ROCK is a downstream effector protein of the small GTPase Rho, which is one of the major regulators of the cytoskeleton.

ROCK Isoform Specific Products:

ROCK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156550
    ROCK-IN-8
    		Inhibitor
    ROCK-IN-8 (Example 4) is a ROCK inhibitor, with an IC50 value less than 100 nM. ROCK-IN-8 has anti-inflammatory activity. ROCK-IN-8 can be used for research of respiratory and gastro-intestinal diseases.
    ROCK-IN-8
  • HY-118046
    GSK2163632A
    		Inhibitor
    GSK2163632A is a selective G protein-coupled receptor kinase (GRK) inhibitor that can be used as a probe for studying heart failure and Parkinson's disease. GSK2163632A potently inhibits GRK1 and GRK5, and also inhibits Rho-associated coiled-coil kinase (ROCK) and insulin-like growth factor receptor IGF-1R. GSK2163632A binds to GRK2 in a manner similar to Paroxetine (HY-122272).
    GSK2163632A
  • HY-164809
    Desisopropyle-belumosudil
    		Inhibitor
    KD025m1 is a novel selective ROCK2 inhibitor. KD025m1 has good anti obesity, improved insulin sensitivity, and blood glucose control effects. KD025m1 can be used to study metabolic diseases such as diabetes and obesity.
    Desisopropyle-belumosudil
  • HY-W110138
    Chloroxoquinoline
    		Inhibitor
    Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer.
    Chloroxoquinoline
  • HY-156593
    ROCK-IN-9
    		Inhibitor
    ROCK-IN-9 (Compound T345) is a ROCK inhibitor. ROCK-IN-9 shows cytotoxicity in HepG2 cell, with an IC50 of 40.8 μM. ROCK-IN-9 has good pharmacokinetic properties in mice, and shows high in vivo exposure and oral bioavailability at lower doses.
    ROCK-IN-9
  • HY-RS12115
    Rock1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Rock1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Rock1 Mouse Pre-designed siRNA Set A
  • HY-P5467
    S6(229-239), Amide, biotinalyted
    		Substrate
    S6(229-239), Amide, biotinalyted is a biological active peptide. (substrate for Rho-Kinase II)
    S6(229-239), Amide, biotinalyted
  • HY-10833
    ROCK-IN-10
    		Inhibitor
    ROCK-IN-10 (compound 50) is a potent ROCK inhibitor with IC50 values of 6 nM and 4 nM for ROCK1 and ROCK2, respectively. ROCK-IN-10 shows >100-fold selectivity against other kinases.
    ROCK-IN-10
  • HY-179498
    ROCK2-IN-13
    		Inhibitor
    ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach.
    ROCK2-IN-13
  • HY-123958
    SB772077B
    		Inhibitor
    SB772077B is a ROCK inhibitor. SB772077B has an anti-inflammatory activity and enhances aqueous outflow facility (OF) by inactivating RhoA/ROCK signal pathway. SB772077B significantly reduces the mRNA level of β-catenin and protein level of fibrotic markers, such as vinculin, fibronectin, collagen 1 A and vimentin. SB772077B also has vasodialatory activity and decreases pulmonary and systemic blood pressure. SB772077B can be used for glaucoma research and pulmonary hypertensive disorder research.
    SB772077B
  • HY-150187
    20:4 Lyso PI
    		Activator
    20:4 Lyso PI acts as an activator of GPR55 and RhoA. 20:4 Lyso PI activates the GPR55-RhoA-ROCK pathway, thereby inducing morphological changes, cytoskeleton assembly, cell rounding and stress fiber formation. 20:4 Lyso PI can be used in research related to diseases such as those of the nervous system.
    20:4 Lyso PI
  • HY-100984A
    HA-100 hydrochloride
    		Inhibitor
    HA-100 hydrochloride is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 hydrochloride also used as a ROCK inhibitor.
    HA-100 hydrochloride
  • HY-N10341
    Centaureidin
    		Activator
    Centaureidin is an orally active IFN-promoter that can be isolated from Bidens pilosa with an EC50 of 0.9 μg/mL. Centaureidin activates the Rho signal pathway, leading to actin and tubulin disassembly, and resulting in dendrite retraction and stress fiber formation in melanocytes. Centaureidin shows high tumor cell growth inhibitory activities. Centaureidin significantly inhibits paw edema in mice[1][2][3][4][5].
    Centaureidin
  • HY-13300A
    SR-3677 dihydrochloride
    		Inhibitor
    SR-3677 dihydrochloride (compound 5) is a potent and selective ROCK-I and ROCK-II inhibitor with an IC50 values of 56 nM and 3 nM.
    SR-3677 dihydrochloride
  • HY-171909
    Glycerophosphoinositol 4-phosphate
    		Activator
    Glycerophosphoinositol 4-phosphate (GroPIns-4-P) is a metabolite of phospholipase A and an inhibitor of adenylylcyclase. Glycerophosphoinositol 4-phosphate can regulate cAMP-dependent cellular functions. Glycerophosphoinositol 4-phosphate can also induce the formation of membrane ruffles and stress fibers in serum-starved Swiss 3T3 cells by activating the small GTPases Rac and Rho, respectively. Glycerophosphoinositol 4-phosphate can be used in research on cancer cell motility and invasiveness.
    Glycerophosphoinositol 4-phosphate
  • HY-12798CR
    AR-13503 (Standard)
    		Inhibitor
    Fluanisone (Standard) is the analytical standard of Fluanisone. This product is intended for research and analytical applications. Fluanisone has potent sedative effect in vivo. Fluanisone can be used to study schizophrenia.
    AR-13503 (Standard)
  • HY-123484
    ROCK-IN-D1
    		Inhibitor
    ROCK-IN-D1 serves as a highly effective and selective inhibitor of ROCK.
    ROCK-IN-D1
  • HY-12798E
    (R)-AR-13503
    		Control 98.20%
    (R)-AR-13503 ((R)-AR-13324 M1 metabolite) is the the (R)-enantiomer of AR-13503 (HY-12798C). AR-13503 is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research.
    (R)-AR-13503
  • HY-145294
    ROCK2-IN-5
    		Inhibitor
    ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation.
    ROCK2-IN-5
  • HY-162596A
    (Rac)-NRL-1049 dihydrochloride
    		Inhibitor
    (Rac)-NRL-1049 is the racemic mixture of NRL-1049 (BA-1049 (free base)) (HY-162596). NRL-1049 is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations.
    (Rac)-NRL-1049 dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
ROCK Isoform Comparison

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