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 | 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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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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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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V2734 | Hydroxyfasudil (HA-1100) | 105628-72-6 | Hydroxyfasudil (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. |
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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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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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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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V79300 | ROCK2-IN-5 | 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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V76489 | Sovesudil hydrochloride (PHP-201 hydrochloride; AMA0076 hydrochloride) | 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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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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