ROCK

<p>ROCK inhibitor-2 is a selective dual inhibitor of ROCK1 and ROCK2 (IC50s of 17 nM and 2 nM, respectively).</p>

<p>Netarsudil Dihydrochloride (AR-13324 Dihydrochloride) is an inhibitor of Rho-related protein kinase (ROCK) and norepinephrine transporter (NET) and is effective in reducing intraocular pressure (IOP).Cost-effective and quality-assured.</p>

<p>Y-33075 dihydrochloride is a selective inhibitor of ROCK(IC50 of 3.6 nM).</p>

<p>CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM).</p>

<p>Akt/ROCK-IN-1 (B12) is a dual inhibitor targeting Akt and ROCK, exhibiting IC50 values of 0.023 nM and 1.47 nM, respectively.</p>

<p>RhoA-ROCK-IN-1 (Compound b19) is an inhibitor of the RhoA/ROCK pathway. It significantly inhibits cell proliferation, migration, and invasion, while promoting cell apoptosis (apoptosis). RhoA-ROCK-IN-1 exhibits strong anticancer activities by inhibiting the RhoA/ROCK pathway.</p>

<p>WAY-656935 inhibits ROCK.</p>

<p>LX-7101 hydrochloride is a potent LIMK and ROCK2 inhibitor with antihypertensive activity, inhibits LIMK1/2, ROCK, PKA, and can be used to study glaucoma.</p>

<p>GKI-1 HCl is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL and hGWL-KinDom.The inhibitory effect of GKI-1 HCl on ROCK1 is more significant.</p>

<p>ROCK2-IN-9 (compound 7u), a selective ROCK2 inhibitor with an IC50 value of 36.8 nM, demonstrates anticancer properties by impeding cancer cell migration and invasion. This action is achieved through the regulation of various actin cytoskeleton cellular activities. It holds potential for use in breast cancer research.</p>

<p>Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.</p>

<p>Ripasudil free base (K-115 (free base)) is a selective and potent ROCK inhibitor, is a novel and potent antiglaucoma agent.</p>

<p>Verosudil (AR-12286), a ROCK1/2 inhibitor (Ki: 2 nM), lowers intraocular pressure in mice by enhancing aqueous outflow.</p>

<p>GSK269962A hydrochloride (GSK 269962 hydrochloride) is a ROCK inhibitor with anti-inflammatory and vasodilatory effects and inhibits ROCK1 and ROCK2.</p>

<p>Cotosudil is a ROCK kinase inhibitor with antihypertensive activity used to treat or prevent neurodegenerative diseases.</p>

<p>Belumosudil mesylate (KD025 mesylate) is a ROCK2 inhibitor with antifibrotic activity, and can be used in chronic graft-versus-host disease research.</p>

<p>GSK180736A: GRK2 inhibitor (IC50 0.77µM), &gt;100x selectivity vs GRKs, weak at PKA (IC50 30µM), strong vs ROCK1 (IC50 100nM).</p>

<p>Thiazovivin, a ROCK inhibitor (IC50: 0.5 μM), increases the survival rate of hESC.</p>

<p>CCG-222740 is an inhibitor of Rho/MRTF pathway</p>

<p>RKI-1447 is a potent inhibitor of ROCK1 and ROCK2. It has anti-invasive and antitumor activities.</p>

<p>Tofacitinib (Tasocitinib) is an orally Janus kinase inhibitor. Tofacitinib is used for the treatment of rheumatoid arthritis. Cost effective and quality assured.</p>

<p>HA-100 is an inhibitor of protein kinase</p>

<p>RKI1313 (RKI-1313) was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion</p>

<p>Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).</p>

<p>GSK429286A (RHO-15) is a specific inhibitor of ROCK1/2 (IC50: 14/63 nM).</p>

<p>SAR407899 hydrochloride is a selective, potent and ATP-competitive ROCK inhibitor, with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and</p>

<p>URMC-099: oral, brain-accessible MLK/LRRK2 inhibitor; IC50 – MLK1/2/3/DLK: 19/42/14/150 nM, LRRK2: 11 nM.</p>

<p>SAR407899 is Rho kinase inhibitor potently inhibits endothelin-1-induced constriction of renal resistance arteries.</p>

<p>CKI-7 is a potent and ATP-competitive inhibitor of casein kinase 1 (CK1; IC50: 6 μM; Ki: 8.5 μM) and a selective Cdc7 kinase inhibitor.</p>

<p>AT13148 is an oral-active and ATP-competitive, multi-AGC kinase inhibitor for Akt1/2/3, p70S6K, PKA, and ROCKI/II.</p>

<p>ROCK-IN-2 (Azaindole 1) is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2.</p>

<p>Narciclasine (Lycoricidinol), a natural product, modulates the Rho/Rho-kinase/LIM kinase/cofilin signaling pathway, greatly increasing GTPase RhoA activity.</p>

<p>ZINC00881524 (ROCK inhibitor) is an effective and specific ROCK inhibitor.</p>

<p>Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.</p>

<p>Afuresertib hydrochloride is an inhibitor of Akt kinase (Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively)</p>

<p>Hydroxyfasudil Hydrochloride (HA 1100 hydrochloride) is a ROCK1/2 inhibitor (IC50s: 0.73/0.72 μM).</p>

<p>Y-27632 (Y-27632) is an orally potent, ATP-competitive inhibitor of ROCK-I and ROCK-II.</p>

<p>Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).</p>

<p>View and buy Y-27632 dihydrochloride from TargetMol.Y-27632 is a selective inhibitor of ROCKs.Cited in 10 publications.</p>

<p>BDP5290 is a potent inhibitor of both ROCK and MRCK(IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.)</p>

<p>Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic</p>

<p>SR-3677 is an effective and specific inhibitor of ROCK2 (IC50: 3 nM).</p>

<p>GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.</p>

<p>GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K, and a dramatically improved P450 profile.</p>

<p>Netarsudil mesylate (AR-13324 mesylate) is a Rho-related protein kinase inhibitor used to study glaucoma and hypertension.</p>

<p>CAY10746 selectively inhibits ROCK I/II with IC50s: 0.014/0.003 μM, useful for diabetic retinopathy research.</p>

<p>H-1152 is a potent, specific, ATP-competitive, and cell permeable ROCK inhibitor (Ki = 1.6 nM).</p>

<p>SB-772077B dihydrochloride is an aminofurazan-based Rho kinase inhibitor (IC50s: 5.6 nM and 6 nM toward ROCK1 and ROCK2, respectively).</p>

<p>Y-33075 (Y-39983 free base) is a ROCK inhibitor that lowers IOP, increases blood flow to ONH, and increases the number of RGCs with regenerating axons.</p>

<p>CID-5056270 has anticancer activity and can inhibit lung cancer, anal cancer, bladder cancer, cervical cancer, vulvar cancer, penile cancer, Burkitt's lymphoma</p>

<p>Rhodblock 6 is a Rho kinase inhibitor, blocking phosphorylated MRLC localization by targeting ROCK activity.</p>

<p>Rho-Kinase-IN-1: ROCK inhibitor, Ki of 30.5 nM (ROCK1) &amp; 3.9 nM (ROCK2), used in research for diseases linked to cell overgrowth and inflammation.</p>

<p>CRT0066854 HCl inhibits atypical PKCs; IC50: PKCι 132 nM, PKCζ 639 nM, ROCK-II 620 nM.</p>

<p>AS 1892802, a ROCK inhibitor: IC50 - 52nM (hROCK2), 57nM (rROCK2), 122nM (hROCK1). Fast antinociceptive effect similar to Tramadol, Diclofenac.</p>

<p>LX7101 is an effective inhibitor of LIMK and ROCK2 (IC50: 24, 1.6, and 10 nM for LIMK1, LIMK2, and ROCK2, respectively). It also inhibits PKA (IC50 &lt;1 nM).</p>

<p>ROCK-IN-7 (compound 9) serves as a ROCK kinase inhibitor and is utilized in the investigation of ocular conditions, including glaucoma and retinal diseases [1].</p>

<p>ROCK-IN-9 (Compound T345), a ROCK inhibitor, exhibits cytotoxicity in HepG2 cells with an IC50 of 40.8 μM.</p>

<p>ROCK2-IN-6 hydrochloride (Comp A)为一种选择性ROCK2抑制剂，适用于研究ROCK介导的疾病、自身免疫性病症与炎症。</p>

<p>Chroman 1 is a potent inhibitor of ROCK1 (IC50 = 52 pM) and ROCK2 (IC50 = 1 pM).</p>

<p>ROCK2-IN-2 is a selective inhibitor of ROCK2 (IC50 of &lt;1 μM).</p>

<p>ROCK-IN-8 (Example 4), a ROCK inhibitor, exhibits anti-inflammatory properties and is suitable for respiratory and gastro-intestinal disease research,</p>

<p>ROCK-IN-1 is a potent ROCK inhibitor that inhibits ROCK2-mediated signaling with an IC50 value of 1.2 nM.ROCK-IN-1 can be used in the study of neurological</p>

<p>H-1152 2HCl: ROCK inhibitor, IC50=12 nM, Ki=1.6 nM. Blocks PKA, PKC, PKG, Aurora A, CaMKII with higher IC50s.</p>

<p>ROCK/HDAC-IN-1 (Compound 10h) serves as an orally effective inhibitor of ROCK/HDAC. This compound suppresses ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). It stimulates the activation of DAMPs, notably calreticulin (CRT) exposure and HMGB1 release, suggesting its potential as an inducer of immunogenic cell death (ICD). ROCK/HDAC-IN-1 exhibits antiproliferative effects against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cells), inhibits tumor growth, activates T cells, and shows no significant toxicity.</p>

<p>ROCK-IN-11 (example 94) is an effective inhibitor of ROCK1 and ROCK2, with an IC50 of ≤ 5 μM, and plays a significant role in cancer research.</p>

<p>Rhodblock 1a is an inhibitor of the Rho kinase signaling pathway, which disrupts the localization and function of proteins within the Rho pathway. This interference hinders the proper formation of the cleavage furrow during cell division, leading to some cells either failing to form the cleavage furrow or forming a ruptured furrow, resulting in binucleated cells. Rhodblock 1a can be utilized for investigating cell division mechanisms and holds potential for research into cardiovascular diseases and cancer.</p>

<p>PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1/PKM1/2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.</p>

<p>Zelasudil (RXC007) is a Rho-related (ROCK) kinase inhibitor for the study of idiopathic pulmonary fibrosis and inflammation.</p>

<p>ROCK2-IN-6 (Comp A) is a selective inhibitor of ROCK2, applicable in the study and treatment of ROCK-mediated, autoimmune, and inflammatory diseases [1].</p>

<p>ROCK-IN-6, a selective ROCK2 inhibitor, exhibits potent inhibition with an IC50 of 2.19 nM and holds promise for research into glaucoma and retinal diseases [1</p>