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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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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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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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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V24575 | LX7101 | 1192189-69-7 | LX7101 (LX-7101;LX 7101)is a novel, potent, pyrrolopyrimidine-based, and topically-usd inhibitor of LIM domain kinase 2 (LIMK2), which isa kinase associated with the regulation of intraocular pressure. |
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V88765 | NRL-1049 | 1973494-16-4 | NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1, respectively). NRL-1049 reduces lysophosphatidic acid-induced ROCK activation in endothelial cells. |
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V88762 | Palmitoyl 3-carbacyclic phosphatidic acid | 476310-22-2 | Palmitoyl 3-carbacyclic phosphatidic acid is a palmitoylated Carba-type cyclic phosphatidic acid, an analog of lysophosphatidic acid (LPA). |
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V93210 | PT109 | 2059104-90-2 | PT109 is a multi-kinase inhibitor that plays an important role in anti-inflammation, anti-oxidation, neurogenesis, synapse formation, etc. by inhibiting JNK (JNK1: IC50=0.143μM; JNK2: IC50=0.831μM; JNK3: IC50=0.285μM) or other kinases (SGK1: IC50=1.34μM; SGK2: IC50=5.6μM; SGK3: IC50=26.4μM; ROCK2: IC50=34μM). |
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V13826 | RKI-1313 | 1342276-76-9 | RKI-1313 is a ROCK inhibitor (antagonist) with IC50s of 34 and 8 µM for ROCK 1 and ROCK 2 respectively. |
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V88764 | ROCK-IN-10 | 1038549-25-5 | ROCK-IN-10 (compound 50) is a potent ROCK inhibitor with IC50 values of 6 nM and 4 nM for ROCK1 and ROCK2, respectively. |
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V79300 | ROCK2-IN-5 | 3031515-48-4 | ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic acid and ferulic acid. |
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V99187 | ROCK2-IN-9 | ROCK2-IN-9 (Compound 7u) is a selective ROCK2 inhibitor with anticancer activity (IC50=36.8 nM). | |
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V76489 | Sovesudil hydrochloride (PHP-201 hydrochloride; AMA0076 hydrochloride) | 2984963-50-8 | Sovesudil (PHP-201) HCl is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor (antagonist) with IC50s of 3.7 and 2.3 nM for ROCK I and ROCK II, respectively. |
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V2951 | SR-3677 | 1072959-67-1 | SR-3677 (SR3677) is a potent and selective Rho-kinase/ROCK2 inhibitor with anticancer activity. |
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V3170 | Netarsudil Mesylate (AR-13324) | 1422144-42-0 | Netarsudil mesylate, the mesylate salt form of Netarsudil (formerly known as AR-13324; Rhopressa), is novel ROCK inhibitor with Ki of 0.2-10.3 nM. |
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V40835 | Belumosudil mesylate (KD025 mesylate) | 2109704-99-4 | Belumosudil mesylate (previously SLx2119; KD025; SLx-2119; KD-025; Rezurock), the mesylate salt of belumosudil, is anorally bioavailable ROCK2 inhibitor approved in 2021 for the treatment of chronic graft versus host disease (cGvHD). |
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V20464 | Verosudil | 1414854-42-4 | Verosudil (AR-11324; AR 11324; AR11324) is a novel and potent Rho kinase inhibitorwith anti-hypertensive activity. |
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V2734 | Hydroxyfasudil (HA-1100) | 105628-72-6 | Hydroxyfasudil (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. |