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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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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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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V53061 | Cotosudil | 1258833-31-6 | Cotosudil is a ROCK kinase inhibitor used in glaucoma or ocular hypertension research. |
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V1344 | Fasudil (HA-1077) HCl | 105628-07-7 | Fasudil HCl(formerly known as HA1077; HA 1077;HA-1077),the hydrochloride salt of fasudil, is a potent multikinase inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with the potential to be used for the treatment of cerebral vasospasm. |
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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. |
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V51967 | Hu7691 | 2360523-76-6 | Hu7691 is an orally bioactive, selective Akt inhibitor (antagonist) with IC50s of 4.0 nM, 97.5 nM and 28 nM for Akt1, Akt2 and Akt3 respectively. |
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V51966 | Hu7691 free base | 2241232-43-7 | Hu7691 free base is an orally bioactive, selective Akt inhibitor (antagonist) with IC50s of 4.0 nM, 97.5 nM and 28 nM for Akt1, Akt2 and Akt3 respectively. |
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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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V2563 | Kobe0065 | 436133-68-5 | Kobe0065 (Kobe 0065) is novel and potent inhibitor of the H-Ras-cRaf1 interaction whichexhibits potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM. |
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V2560 | Netarsudil 2HCl (AR-13324) | 1253952-02-1 | Netarsudil 2HCl (formerly AR13324; AR 13324;AR-13324;Rhopressa), the dihydrochloride salt ofNetarsudil, is ROCK inhibitor with antihypertensive activity and the potential for glaucoma treatment. |
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V2564 | PD0166285 | 185039-89-8 | PD0166285 (PD-0166285) is a novel and potent Wee1 and Chk1 inhibitor with anticancer activity and enzymatic activity at nanomolar concentrations (IC50s of 24 and 72 nM for WEE1 and Myt1, respectively). |
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V1348 | Ripasudil (K-115) HCl dihydrate | 887375-67-9 | Ripasudil HCl dihydrate (formerly K-115; K-115; trade name: Glanatec),the hydrochloride salt and hydrated form of ripasudil, is a ROCK1/2 inhibitor with antihypertensive effects. |
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V2562 | RK-33 | 1070773-09-9 | RK-33 is a potent and first-in-class small molecule inhibitor of DDX3 (a RNA helicase) and causes G1 cell cycle arrest, induces apoptosis, and promotes radiation sensitization in DDX3-overexpressing cells. |
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