rho-kinase

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.

Rho-Kinase-IN-2 (Compound 23) is an orally active and selective inhibitor of Rho Kinase (ROCK) with CNS penetration, exhibiting a high affinity for ROCK2 with an IC50 of 3 nM. This compound is of potential interest for further investigations in Huntington's disease research [1].

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.

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.

Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) activates signal-transducing G proteins involved in cellular processes such as proliferation, differentiation, and activation of intracellular kinase cascades. It regulates proliferation and apoptosis through the hydrolysis by small GTPases Ras and Rho, and plays a role in vesicle docking, fusion, and formation via Rab. Additionally, GTP serves as an energy-rich precursor for the biosynthesis of DNA and RNA.

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

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

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.

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).

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).

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

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

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

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.

HA-100 is an inhibitor of protein kinase

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.

ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 17 nM and 2 nM, respectively.

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

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).

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

ROCK2-IN-2 is a selective inhibitor of ROCK2, with an IC50 of less than 1 μM.

Y-33075 dihydrochloride is a selective inhibitor of ROCK with an IC50 of 3.6 nM.

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.

GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).

SAR407899 hydrochloride 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.

RKI1313 (RKI-1313) was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.

GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).

ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.

Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50 Ki: 60 41 nM).

ZINC00881524 (ROCK inhibitor) is an effective and specific ROCK inhibitor.

SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.

Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive Rho kinase (ROCK) inhibitor, acting on ROCK I (IC50: 3.7 nM) and ROCK II (IC50: 2.3 nM), and lowers IOP without causing congestion.

CAY10746 is a selective Rho kinase (ROCK) inhibitor, targeting ROCK I and ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be employed in the study of diabetic retinopathy.

ROCK2-IN-5, a compound integrating structural elements from the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids, exhibits a favorable multitarget profile and tolerability. It shows potential for research in Amyotrophic Lateral Sclerosis (ALS) associated with a SOD1 mutation.

Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor, showing IC50 values of 3.7 nM for ROCK-I and 2.3 nM for ROCK-II, and capable of lowering intraocular pressure (IOP) without inducing hyperemia.

AR-13503, is an metabolite of Netarsudil (AR-11324), is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure.

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.

ROCKII-IN-DI is a potent, competitive inhibitor of Rho-associated coiled-coil-containing protein kinase 2 (ROCKII).

NSC-2488 is a novel Rho-Kinase-II Inhibitor with Vasodilatory Activity.

AR-13324 analog mesylate, an inhibitor of Rho-kinase and the norepinephrine transporter, reduces intraocular pressure in normotensive monkey eyes.

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

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

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

PT-262 is a ROCK (Rho-associated coiled-coil forming protein kinase) inhibitor. It induces cytoskeleton remodeling and migration inhibition in lung carcinoma cells.

Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

BIPM is a potent inhibitor of Rho-associated protein kinase 2 (ROCK2). Exposure of SH-SY5Y cells to BIPM led to significant changes in cell migration, actin stress fibers and neurite length. BIPM significantly inhibits phosphorylation of cofilin, a regula

LX7101 is a potent inhibitor of both LIM kinase (LIMK) 1 and 2, and Rho-associated kinase 1 (ROCK1) and ROCK2, with IC50 values of 32, 4.3, 69, and 32 nM, respectively. It is selective, demonstrated by its lack of cross-reactivity in a panel of binding assays involving 78 receptors, transporters, and an additional 430 kinases, at a concentration of 10 μM. The topical administration of LX7101 (3 μl of a 1 mg/ml solution) to the eye has been shown to reduce intraocular pressure in a dexamethasone-induced mouse model of glaucoma.

NSC-4231 is a novel Rho-Kinase-II Inhibitor with Vasodilatory Activity.