ROCK

ROCK

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.

ROCK related products

Structure Cat No. Product Name CAS No. Product Description
V77245 AR-13324 analog mesylate
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.
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).
V79028 Chroman 1 dihydrochloride
V2734 Hydroxyfasudil (HA-1100) 105628-72-6 Hydroxyfasudil (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
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.
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.
V13826 RKI-1313 1342276-76-9 RKI-1313 is a novel and potent inhibitor of the ROCK kinases.
V79300 ROCK2-IN-5
V76489 Sovesudil hydrochloride (PHP-201 hydrochloride; AMA0076 hydrochloride)
V2951 SR-3677 1072959-67-1 SR-3677 (SR3677) is a potent and selective Rho-kinase/ROCK2 inhibitor with anticancer activity.
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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