The AGC (PKA/PKG/PKC) family of serine-threonine kinases includes ROCK (Rho-associated protein kinase). Animals such as chicken, zebrafish, Xenopus, and mammals also have ROCKs (ROCK1 and ROCK2). With a molecular weight of 158 kDa, human ROCK1 is a significant RhoA small GTPase downstream effector. A kinase domain, an acoiled-coil region, and a Pleckstrin homology (PH) domain make up a mammalian ROCK. If RhoA-GTP is absent, the kinase activity of ROCKs is reduced by an autoinhibitory intramolecular fold. Since ROCK is a downstream effector protein of the small GTPase Rho, one of the primary regulators of the cytoskeleton, ROCK is involved in a variety of different cellular phenomena.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V114421 | (Rac)-NRL-1049 dihydrochloride | 863638-93-1 | (Rac)-BA 1049 is a racemic variant of NRL-1049 (BA-1049). |
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V118982 | 5-Nitro-1H-indazole-3-carbonitrile | 90348-29-1 | 5-Nitro-1H-indazole-3-nitrile (DL0805) is a Rho kinase (ROCK) inhibitor with an IC50 value of 6.67 μM against ROCK-I. |
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V77245 | AR-13324 analog mesylate | 2095432-73-6 | AR-13324 analog mesylate is an analog of AR-13324. |
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V32183 | BDP5290 | 1817698-21-7 | BDP5290 is a novel, potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively. |
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V35094 | CaMKP inhibitor sodium | 52789-62-5 | CaMKP inhibitor sodium is a selective ROCK1 inhibitor (antagonist) with IC50 of 14 nM. |
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V52297 | CAY10746 | 2247240-76-0 | CAY10746 is a selective Rho kinase (ROCK) inhibitor. |
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V131373 | Centaureidin | 17313-52-9 | Centaureidin is an orally effective interferon agonist isolated from Bidens pilosa, with an EC50 value of 0.9 μg/mL. |
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V79028 | Chroman 1 dihydrochloride | Chroman 1 di-HCl is a potent and specific ROCK inhibitor (antagonist) with stronger effect on ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). | |
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V88767 | CMPD101 hydrochloride | 1941168-71-3 | CMPD101 hydrochloride, a membrane permeable, small molecule inhibitor of GRK2 and GRK3 with IC50 values of 18 nM and 5.4 nM, respectively. |
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V53061 | Cotosudil | 1258833-31-6 | Cotosudil is a ROCK kinase inhibitor used in glaucoma or ocular hypertension research. |
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V115227 | Desisopropyle-belumosudil | 911417-89-5 | Deisopropyl-beromosudil (compound 84) is a ROCK inhibitor (IC50 of 2.6 μM for ROCK 1 and 0.52 μM for ROCK 2). |
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V88763 | DJ4 | 1681020-24-5 | DJ4 is an ATP-competitive inhibitor of ROCK1/2 (IC50 values: 5 and 50 nM) and MRCKα/β (IC50 values: 10 and 100 nM). |
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V136770 | Glycerophosphoinositol 4-phosphate disodium | Glycerophosphoinositol 4-phosphate disodium is a metabolite of phospholipase A and an inhibitor of adenylate cyclase. | |
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V55052 | Glycyl H-1152 hydrochloride | 913844-45-8 | Glycyl H-1152 HCl is a glycosyl analogue of the Rho-kinase inhibitor H-1152 di-HCl. |
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V2730 | GSK180736A | 817194-38-0 | GSK180736A (GSK-180736A) is a GRK2 inhibitor thatwasdeveloped as a novel and potent Rho-associated, coiled-coil-containing protein kinase (ROCK) inhibitor whichbinds to GRK2 (G protein-coupled receptor kinase 2) with IC50of 0.77 μM; G protein-coupled receptors (GPCRs) are central to many physiological processes. |
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V2561 | GSK269962 (GSK269962A) | 850664-21-0 | GSK269962 (also known as GSK269962A) is a novel, potent and selective inhibitor of ROCK (Rho-associated protein kinase) with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively. |
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V3320 | GSK269962 HCl | 2095432-71-4 | GSK269962 HCl (also called GSK-269962A HCl),the hydrochloride salt ofGSK 269962A, is a selective ROCK (Rho-associated protein kinase) inhibitor with potential antihypertensive and cardioprotective activity. |
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V1345 | GSK429286A | 864082-47-3 | GSK429286A (also known as RHO15;GSK 429286A;RHO-15;GSK-429286A)is a potent, orally bioactive, andselective inhibitor of ROCK1/2 with antihypertensive effects. |
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V67533 | HA-100 dihydrochloride | 210297-47-5 | HA-100 di-HCl is a potent protein kinase inhibitor (antagonist) with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for PKG, PKA, PKC and MLC kinases respectively. |
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V52021 | HA-100 hydrochloride | 141543-63-7 | HA-100 HCl is a potent protein kinase inhibitor (antagonist) with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for PKG, PKA, PKC and MLC kinases, respectively. |