ROCK

Rho-associated protein kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. It is involved mainly in regulating the shape and movement of cells by acting on the cytoskeleton.ROCKs (ROCK1 and ROCK2) occur in mammals (human, rat, mouse, cow), zebrafish, Xenopus, invertebrates (C. elegans, mosquito, Drosophila) and chicken. Human ROCK1 has a molecular mass of 158 kDa and is a major downstream effector of the small GTPase RhoA. Mammalian ROCK consists of a kinase domain, a coiled-coil region and a Pleckstrin homology (PH) domain, which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular fold if RhoA-GTP is not present.

产品编号	产品名称
T2155	ThiazovivinHOT	Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC.
T1725	Y-27632 dihydrochlorideHOT	Y-27632 is a selective inhibitor of ROCKs including p160ROCK (Ki: 140 nM) and ROCK2 (IC50: 800 nM).
T4276L	Hydroxyfasudil	Hydroxyfasudil is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).
T3513	GSK180736A	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)...
T4095	ZINC00881524	ZINC00881524 is an effective and specific ROCK inhibitor.
T4276	Hydroxyfasudil Hydrochloride	Hydroxyfasudil hydrochloride is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).
T6867	KD025	KD025 is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).
T2633	GSK429286A	GSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
T3518	GSK269962A	GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
T1870	Y27632	Y-27632 is a selective ATP-competitive inhibitor of ROCK-I and ROCK-II.
T6321	Tofacitinib	Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T7301	BDP5290	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.)
T1898	RKI1447	RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.
T2011	RKI1313	RKI-1313 was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.
T2482	AT13148	AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
T3060	Fasudil hydrochloride	Fasudil Hydrochloride 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.
T7492	Ripasudil free base	Ripasudil free base is a selective and potent ROCK inhibitor, is a novel and potent antiglaucoma agent.
T7552	H-1152	H-1152 is a potent, specific, ATP-competitive, and cell permeable ROCK inhibitor (Ki = 1.6 nM).
T16855	SB-772077B dihydrochloride	SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively).
T14960	Chroman 1	Chroman 1 is an inhibitor of ROCK2 (IC50: 1 nM).
T10358	Netarsudil hydrochloride	Netarsudil hydrochloride is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IO...
T15808	Merestinib dihydrochloride	Merestinib dihydrochloride is an effective and orally bioavailable c-Met inhibitor (Ki=2 nM). It has anti-tumor activities and also has potent activity against ...
T13424	(1R,2S)-VU0155041	(1R,2S)-VU0155041 is a partial agonist of mGluR4(EC50 of 2.35 μM).
T13364	YAP/TAZ inhibitor-1	YAP/TAZ inhibitor-1 is an inhibitor of YAP/TAZ (IC50 of <0.100 μΜ in firefly luciferase assay).
T13972	Y-9738	Y-9738 is an agent of hypolipidemic.
T14989	CMPD101	CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits...
T12747	ROCK2-IN-2	ROCK2-IN-2 is a selective inhibitor of ROCK2(IC50 of <1 μM).
TQ0110	Azaindole 1	Azaindole 1 (TC-S 7001) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.
T12746	ROCK inhibitor-2	ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).
T12721	Rho-Kinase-IN-1	Rho-Kinase-IN-1 is a inhibitor of Rho kinase (ROCK) with Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively
TN1533	Cucurbitacin A	Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin/phospho-myosin II co-aggregates by stimulation of the RhoA/R...
TQ0319	Ripasudil hydrochloride dihydrate	Ripasudil (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).
TQ0187	SR-3677	SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).
TQ0183	Narciclasine	Narciclasine, a natural product, modulates the Rho/Rho-kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity.
T1606	Fasudil	Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.