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Cell Cycle/Checkpoint ROCK

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.
Cat No. Product Name
T1725 Y-27632 dihydrochlorideHOT Y-27632 is a selective inhibitor of ROCKs including p160ROCK (Ki: 140 nM) and ROCK2 (IC50: 800 nM).
T1898 RKI-1447 RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.
T1920 CapivasertibHOT Capivasertib (AZD5363) is a new-type orally available inhibitor of the serine/threonine protein kinase AKT (IC50s: 3/7/7 nM for Akt1/2/3).
T2011 RKI-1313 RKI-1313 was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.
T2155 ThiazovivinHOT Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC.
T2398 Tofacitinib CitrateHOT Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
T2482 AT13148 AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
T2633 GSK429286A GSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
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.
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)...
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.
T4095 ZINC00881524 ZINC00881524 is an effective and specific ROCK inhibitor.
T6057 URMC-099 URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM...
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T6867 KD025 KD025 is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).
T4276 Hydroxyfasudil Hydrochloride Hydroxyfasudil hydrochloride is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).
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.)
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).
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.
TQ0183 Narciclasine Narciclasine, a natural product, modulates the Rho/Rho-kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity.
TQ0187 SR-3677 SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: ~3 nM).
TQ0319 Ripasudil hydrochloride dihydrate Ripasudil (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).
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...
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
T12746 ROCK inhibitor-2 ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).
T12747 ROCK2-IN-2 ROCK2-IN-2 is a selective inhibitor of ROCK2(IC50 of <1 μM).
T14960 Chroman 1 Chroman 1 is an inhibitor of ROCK2 (IC50: 1 nM).
T14989 CMPD101 CMPD101 is a membrane-permeable inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM) used for the study of heart failure. CMPD101 exhibits less selectively against GRK1...
T13972 Y-9738 Y-9738 is an agent of hypolipidemic.
T13364 YAP/TAZ inhibitor-1 YAP/TAZ inhibitor-1 is an inhibitor of YAP/TAZ (IC50 of <0.100 μΜ in firefly luciferase assay).
T13424 (1R,2S)-VU0155041 (1R,2S)-VU0155041 is a partial agonist of mGluR4(EC50 of 2.35 μM).
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 ...
T10358 Netarsudil hydrochloride Netarsudil hydrochloride is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IO...
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).
Y-27632 dihydrochloride HOT
T1725CAS 129830-38-2
Y-27632 is a selective inhibitor of ROCKs including p160ROCK (Ki: 140 nM) and ROCK2 (IC50: 800 nM).
RKI-1447
T1898CAS 1342278-01-6
RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.
Capivasertib HOT
T1920CAS 1143532-39-1
Capivasertib (AZD5363) is a new-type orally available inhibitor of the serine/threonine protein kinase AKT (IC50s: 3/7/7 nM for Akt1/2/3).
RKI-1313
T2011CAS 1342276-76-9
RKI-1313 was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.
Thiazovivin HOT
T2155CAS 1226056-71-8
Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC.
Tofacitinib Citrate HOT
T2398CAS 540737-29-9
Tofacitinib citrate is a a potent, cell-permeable inhibitor of JAK1/2/3 (IC50s: 1/20/112 nM).
AT13148
T2482CAS 1056901-62-2
AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.
GSK429286A
T2633CAS 864082-47-3
GSK429286A is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).
Fasudil hydrochloride
T3060CAS 105628-07-7
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.
GSK180736A
T3513CAS 817194-38-0
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)...
GSK269962A
T3518CAS 850664-21-0
GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
ZINC00881524
T4095CAS 557782-81-7
ZINC00881524 is an effective and specific ROCK inhibitor.
URMC-099
T6057CAS 1229582-33-5
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM...
Tofacitinib
T6321CAS 477600-75-2
Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
KD025
T6867CAS 911417-87-3
KD025 is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).
Hydroxyfasudil Hydrochloride
T4276CAS 155558-32-0
Hydroxyfasudil hydrochloride is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).
BDP5290
T7301CAS 1817698-21-7
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.)
Ripasudil free base
T7492CAS 223645-67-8
Ripasudil free base is a selective and potent ROCK inhibitor, is a novel and potent antiglaucoma agent.
H-1152
T7552CAS 451462-58-1
H-1152 is a potent, specific, ATP-competitive, and cell permeable ROCK inhibitor (Ki = 1.6 nM).
Azaindole 1
TQ0110CAS 867017-68-3
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.
Narciclasine
TQ0183CAS 29477-83-6
Narciclasine, a natural product, modulates the Rho/Rho-kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity.
SR-3677
TQ0187CAS 1072959-67-1
SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: ~3 nM).
Ripasudil hydrochloride dihydrate
TQ0319CAS 887375-67-9
Ripasudil (K-115) hydrochloride dihydrate is a specific ROCK inhibitor (IC50s: 51/19 nM for ROCK1/ROCK2).
Cucurbitacin A
TN1533CAS 6040-19-3
Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin/phospho-myosin II co-aggregates by stimulation of the RhoA/R...
Rho-Kinase-IN-1
T12721CAS 1035094-83-7
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
ROCK inhibitor-2
T12746CAS 1127308-52-4
ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).
ROCK2-IN-2
T12747CAS 1995065-79-6
ROCK2-IN-2 is a selective inhibitor of ROCK2(IC50 of <1 μM).
Chroman 1
T14960CAS 1273579-40-0
Chroman 1 is an inhibitor of ROCK2 (IC50: 1 nM).
CMPD101
T14989CAS 865608-11-3
CMPD101 is a membrane-permeable inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM) used for the study of heart failure. CMPD101 exhibits less selectively against GRK1...
Y-9738
T13972CAS 59399-41-6
Y-9738 is an agent of hypolipidemic.
YAP/TAZ inhibitor-1
T13364CAS 2093565-23-0
YAP/TAZ inhibitor-1 is an inhibitor of YAP/TAZ (IC50 of <0.100 μΜ in firefly luciferase assay).
(1R,2S)-VU0155041
T13424CAS 1263273-14-8
(1R,2S)-VU0155041 is a partial agonist of mGluR4(EC50 of 2.35 μM).
Merestinib dihydrochloride
T15808CAS 1206801-37-7
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 ...
Netarsudil hydrochloride
T10358CAS 1253952-02-1
Netarsudil hydrochloride is an inhibitor of Rho-associated protein kinase (ROCK) and norepinephrine transporter (NET) with effective in intraocular pressure (IO...
SB-772077B dihydrochloride
T16855CAS 607373-46-6
SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively).