rho kinase in 1

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.

PKN1 2-IN-1 is a potent and selective PKN2 inhibitor with 14-fold higher selectivity for PKN2 than PKN1, membrane permeability and anticancer potential.Protein kinase N proteins (PKN1, PKN2 and PKN3) are effectors of Rho GTPases and are critical for survival in several tumor cell lines including prostate and breast cancer.

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].

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.

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.

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.