rock2 in 2

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

PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1 PKM1 2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.

ROCK HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).

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

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.

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].

This novel compound is an orally bioavailable antagonist of P2X3 P2X2 3 receptors, exhibiting potent activity with a pIC50 of 8 in both human and rat, and a pIC50 of 7.3 specifically for the human P2X2 3 receptor. It demonstrates high brain penetration, evidenced by a brain to plasma ratio of 6, and effectively blocks agonist-evoked intracellular Ca2+ flux and inward currents within the nanomolar range (10 nM to 1 µM) in cell lines that express human P2X3 and P2X2 3 receptors recombinantly. The compound also shows favorable pharmacokinetic properties, with a half-life (t1 2) of 1.63 hours and a time to reach maximum concentration (Tmax) of 30 minutes.

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.

Nocarnickelamides B (Compound 2) is a linear peptide and an inhibitor of ROCK1 2. It exhibits dual inhibitory activity against ROCK1 and ROCK2, with IC50 values of 14.9 μM and 21.9 μM, respectively. This compound binds to the ATP binding site and inhibits ROCK-mediated cytoskeletal contraction markers, such as myosin light chain activation. Nocarnickelamides B can be utilized in glaucoma research.

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.