rock1

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

Akt/ROCK-IN-1 (B12) is a dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively. It possesses antitumor efficacy against neuroblastoma [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.

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

GKI-1 HCl is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL and hGWL-KinDom.The inhibitory effect of GKI-1 HCl on ROCK1 is more significant.

GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.

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

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

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.

GKI-1 is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL with an IC50 of 4.9. GKI-1 also inhibited hGWL-KinDom, and its IC50 was 2.5 µM. The inhibitory effect of GKI-1 on ROCK1 was better than that of hGWLFL and hGWL-KinDom, and its IC50 was 11 µM, which only weakly inhibited PKA.

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).

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).

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.

THK01, a potent ROCK2 inhibitor, exhibits IC50 values of 5.7 nM for ROCK2 and 923 nM for ROCK1, respectively. It effectively targets the ROCK2-STAT3 signaling pathway to inhibit breast cancer metastasis, making it valuable for breast cancer 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.

Hu7691 free base is an orally active, potent and selective Akt inhibitor with anti-proliferative and neurogenic effects on a variety of neuroblastoma cell lines.Hu7691 free base inhibits Akt1, Akt2, and Akt3 and induces differentiation of neuroblastoma cells.

ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).

ROCK1-IN-1 is an inhibitor of ROCK1 with a K i value of 540 nM. ROCK1-IN-1 can be used in the research of hypertension, glaucoma and erectile dysfunction [1].

GSK269962A hydrochloride (GSK 269962 hydrochloride) is a highly potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.6 nM and 4 nM, respectively, for recombinant human isoforms. This compound exhibits both anti-inflammatory and vasodilatory properties.

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

Belumosudil mesylate (KD025 mesylate) is a compound that selectively inhibits ROCK2, demonstrating IC50 values of 105 nM for ROCK2 and 24 μM for ROCK1. It possesses anti-fibrotic properties.

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.

Hu7691 is an orally active, selective and potent Akt inhibitor that inhibits Akt1, Akt2 and Akt3, inhibits proliferation of neuroblastoma cells and induces differentiation of neuroblastoma cells.

Uprosertib hydrochloride is a potent and selective inhibitor of pan-Akt (IC50: 180/328/38 nM for Akt1/Akt2/Akt3, respectively).

RKI 1447 dihydrochloride is an effective and selective ROCK inhibitor (ROCK1 IC50=14.5 nM, ROCK2 IC50=6.2 nM). RKI 1447 dihydrochloride can inhibit the growth of colorectal cancer cells and promote cell apoptosis.

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.

ATP-competitive ROCK inhibitor

SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively).

BDP5290 is a potent inhibitor of both ROCK and MRCK(IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.)

Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].

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).

ROCK-IN-10 (compound 50) serves as a powerful inhibitor of ROCK, exhibiting IC50 values of 6 nM for ROCK1 and 4 nM for ROCK2, respectively. It demonstrates over 100-fold selectivity towards ROCK1 and ROCK2 when compared to other kinases [1].

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

HSD1590 is a highly effective and potent inhibitor of ROCK1 and ROCK2, with IC50 values of 1.22 nM and 0.51 nM, respectively. It demonstrates exceptional binding affinity to ROCK, with Kd values below 2 nM. Moreover, HSD1590 showcases minimal cytotoxicity, making it an ideal compound for various applications.

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

AKT-IN-3 is a potent, orally active low hERG blocking Akt inhibitor (IC50: 1.4 nM, 1.2 nM, and 1.7 nM for Akt1, Akt2, and Akt3). AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1

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

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

TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM, and shows selectivity >250-fold for CK2 over JNK3, ROCK1, and MET(IC50> 10 uM).

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

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

SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).

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.

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

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.

Chroman 1 dihydrochloride is a selective and potent inhibitor of ROCK, acting more strongly on ROCK2 (IC50: 1 pM) than ROCK1 (IC50: 52 pM) and also inhibiting MRCK activity (IC50: 150 nM).