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 |
|---|---|---|---|---|
|
V114421 | (Rac)-NRL-1049 dihydrochloride | 863638-93-1 | (Rac)-BA 1049 is a racemic variant of NRL-1049 (BA-1049). |
|
V118982 | 5-Nitro-1H-indazole-3-carbonitrile | 90348-29-1 | 5-Nitro-1H-indazole-3-nitrile (DL0805) is a Rho kinase (ROCK) inhibitor with an IC50 value of 6.67 μM against ROCK-I. |
|
V77245 | AR-13324 analog mesylate | 2095432-73-6 | AR-13324 analog mesylate is an analog of AR-13324. |
|
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. |
|
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). | |
|
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. |
|
V115227 | Desisopropyle-belumosudil | 911417-89-5 | Deisopropyl-beromosudil (compound 84) is a ROCK inhibitor (IC50 of 2.6 μM for ROCK 1 and 0.52 μM for ROCK 2). |
|
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). |
|
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. |
|
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. |
|
V111890 | NRL-1049 dihydrochloride | 1973494-17-5 | NRL-1049 dihydrochloride (BA-1049) is a selective, orally effective inhibitor of Rho-associated protein kinase 2 (ROCK2) with an IC50 value of 0.59 μM. |
|
V117082 | NSC126188 | 31863-82-8 | NSC126188 is a RhoB inducer. |
|
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). |
|
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). |
|
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. |
|
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. |
|
V118285 | ROCK2-IN-10 | ROCK2-IN-10 is a highly effective and selective ROCK2 inhibitor (IC50 = 0.020 μM), with a ROCK2 selectivity that is 41 times greater than that of the ROCK1 subtype. | |
|
V118312 | ROCK2-IN-11 | ROCK2-IN-11 (compound A20) is a selective ROCK2 inhibitor with an IC50 of 0.18 μM for ROCK2, which is superior to its inhibitory efficacy against ROCK1. | |
|
V116709 | ROCK2-IN-12 | 3086603-12-2 | ROCK2-IN-12 (compound A25) is a selective ROCK2 inhibitor with an IC50 value of 7.0 nM for ROCK2 and even better inhibitory effect on ROCK1. |
|
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. |