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.

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.

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

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-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.

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).

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.

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

H-1152 is a potent, specific, ATP-competitive, and cell permeable ROCK inhibitor (Ki = 1.6 nM).

Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08 2 2.6 nM for Akt1 Akt2 Akt3 respectively)

ROCK-IN-6, a selective ROCK2 inhibitor, exhibits potent inhibition with an IC50 of 2.19 nM and holds promise for research into glaucoma and retinal diseases [1].

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

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].

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].

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

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.