ROCK

ROCK-IN-5 (compound I-B-37) is a potent inhibitor of protein kinases, including ROCK, ERK, GSK, and AGC, with potential applications in cardiac, proliferative, and neurodegenerative disease research.

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 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.

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

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

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).

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

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).

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

Netarsudil mesylate (AR-13324 mesylate) is a Rho-related protein kinase inhibitor used to study glaucoma and hypertension.

Y-33075 (Y-39983 free base) is a ROCK inhibitor that lowers intraocular pressure (IOP), increases blood flow to the optic nerve head (ONH), and increases the number of RGCs (retinal ganglion cells) in the body with regenerating axons.

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

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

ROCK-IN-11 (example 94) is an effective inhibitor of ROCK1 and ROCK2, with an IC50 of ≤ 5 μM, and plays a significant role in cancer research.

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).

ROCK-IN-12 (compound R3) is a selective inhibitor of ROCK, utilized in glaucoma research.

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.

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

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

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.

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

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

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

BDP5290 is a potent inhibitor of both ROCK and MRCK, with IC50 values of 5 nM for ROCK1, 50 nM for ROCK2, 10 nM for MRCKα, and 100 nM for MRCKβ.