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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V2733 | Hydroxyfasudil HCl (HA1100) | 155558-32-0 | Hydroxyfasudil HCl (also called HA1100 HCl), ametabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator. |
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V1347 | Belumosudil (KD025, SLx-2119) | 911417-87-3 | Belumosudil (formerly known as KD-025,ROCK inhibitor, and SLx-2119; trade name Rezurock) is a novel, potent, orally bioavailable, and selective small molecule ROCK2 inhibitor that has been approved by FDA in July 2021 for the treatment of chronic graft versus host disease (cGvHD). |
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