ROCK

Y-27632 dihydrochloride (Y-27632 2HCl) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 dihydrochloride also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II. Y-27632 also inhibits isolation-induced apoptosis in mouse prostate stem or progenitor cells.

Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IOP) reduction.

Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC.

CID-5056270 has anticancer activity and can inhibit lung cancer, anal cancer, bladder cancer, cervical cancer, vulvar cancer, penile cancer, Burkitt's lymphoma, breast cancer and bone cancer. It can be used to study hypertension, Alzheimer's disease and arteriosclerosis.

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

GKI-1 HCl is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL and hGWL-KinDom.The inhibitory effect of GKI-1 HCl on ROCK1 is more significant.

Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits the localization of phosphorylated MRLC (Myosin Regulatory Light Chain) and acts by specifically inhibiting Rho kinase activity.

WAY-656935 inhibits ROCK.

SB-747651A dihydrochloride is a chemical compound that serves as an ATP-competitive inhibitor for mitogen- and stress-activated kinase 1 (MSK1), featuring an IC50 of 11 nM. Additionally, this compound effectively inhibits PRK2, RSK1, p70S6K, and ROCK-II, showcasing its potential in inflammation research [1].

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC. ROCK-IN-5 exhibits the potential for cardiac, proliferative and neurodegenerative diseases research.

H-1152 dihydrochloride (H-1152 2HCl) is a specific inhibitor of Rho-associated protein kinase (ROCK) with an IC50 of 12 nM and a Ki of 1.6 nM. H-1152 dihydrochloride inhibits PKA, PKC, PKG, Aurora A and CaMKII with IC50 values of 3.03 μM, 5.68 μM, 0.360 μM, 0.745 μM and 0.180 μM, respectively.

CRT0066854 hydrochloride is an effective selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively.

Rho-Kinase-IN-1 is an inhibitor of ROCK with Kis of 30.5 nM and 3.9 nM for ROCK1 and ROCK2, respectively. Rho-Kinase-IN-1 can be used in studies about excessive cell proliferation, remodeling, edema and inflammation diseases.

LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 <1 nM).

Chroman 1 is an inhibitor of ROCK2 (IC50: 1 nM).

Tofacitinib (Tasocitinib) is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).

Ripasudil (Ripasudil hydrochloride dihydrate) (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

YAP/TAZ inhibitor-1 is an inhibitor of YAP/TAZ (IC50 of <0.100 μΜ in firefly luciferase assay).

ROCK2-IN-2 is a selective inhibitor of ROCK2 (IC50 of <1 μM).

ROCK2 inhibitor is a chemical compound associated with the therapeutic management of psoriasis. It exhibits its efficacy in targeting ROCK2 enzymes within HaCaT cells and has demonstrated beneficial effects in a psoriasis-like mouse model.

CCG-232964 is an orally active Rho/MRTF/SRF inhibitor that suppresses LPA-induced CTGF gene expression [1].

Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin/phospho-myosin II co-aggregates by stimulation of the RhoA/ROCK pathway and inhibition of LIM-Kinase.

ROCK-IN-8 (Example 4), a ROCK inhibitor, exhibits anti-inflammatory properties and is suitable for respiratory and gastro-intestinal disease research, demonstrating an IC50 value below 100 nM [1].

ROCK2-IN-6 (Comp A) is a selective inhibitor of ROCK2, applicable in the study and treatment of ROCK-mediated, autoimmune, and inflammatory diseases [1].

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

Y-9738 is an agent of hypolipidemic.

CAY10746 is a selective Rho kinase (ROCK) inhibitor that inhibits ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively.CAY10746 can be used to study diabetic retinopathy.

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).

Ripasudil free base (K-115 (free base)) is a selective and potent ROCK inhibitor, is a novel and potent antiglaucoma agent.

Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).

SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).

Narciclasine (Lycoricidinol), a natural product, modulates the Rho/Rho-kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity.

AS 1892802 is a potent and selective inhibitor of ROCK. AS 1892802 exibits IC50 values of 52nM, 57nM and 122 nM for human ROCK2, rat ROCK2 and human ROCK1, respectively. The onset of antinociceptive effect of AS 1892802 is as fast as those of Tramadol and Diclofenac.

Akt/ROCK-IN-1 (B12) is a dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. It possesses antitumor efficacy against neuroblastoma [1].

RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.

AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.

Verosudil (AR-12286) is a highly potent Rho kinase (ROCK) inhibitor with a Ki of 2 and 2 nM against ROCK1 and ROCK2, respectively. AR-12286 reverses steroid-induced intraocular pressure in mice by decreasing intraocular pressure by increasing outflow of aqueous ether through the trabecular reticulum.

Cotosudil is a ROCK kinase inhibitor with antihypertensive activity and is used to treat or prevent diseases or conditions caused by cataracts, cardiovascular or neurodegenerative diseases or nerve damage.

Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), RO

Y-33075 dihydrochloride is a selective inhibitor of ROCK(IC50 of 3.6 nM).

ROCK-IN-9 (Compound T345), a ROCK inhibitor, exhibits cytotoxicity in HepG2 cells with an IC50 of 40.8 μM. It demonstrates favorable pharmacokinetic properties in mice, achieving high in vivo exposure and oral bioavailability at low doses [1].

ROCK-IN-7 (compound 9) serves as a ROCK kinase inhibitor and is utilized in the investigation of ocular conditions, including glaucoma and retinal diseases [1].

CKI-7 is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1), and MSK1.

ROCK-IN-1 is a potent ROCK inhibitor that inhibits ROCK2-mediated signaling with an IC50 value of 1.2 nM.ROCK-IN-1 can be used in the study of neurological disorders and inflammation-related diseases.