yingweiwo

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
AR-13324 analog mesylate V77245 AR-13324 analog mesylate 2095432-73-6 AR-13324 analog mesylate is an analog of AR-13324.
BDP5290 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.
Chroman 1 dihydrochloride 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).
CMPD101 hydrochloride 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.
DJ4 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).
LX7101 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.
NRL-1049 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.
Palmitoyl 3-carbacyclic phosphatidic acid 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).
PT109 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).
RKI-1313 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.
ROCK-IN-10 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.
ROCK2-IN-5 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.
ROCK2-IN-9 V99187 ROCK2-IN-9 ROCK2-IN-9 (Compound 7u) is a selective ROCK2 inhibitor with anticancer activity (IC50=36.8 nM).
Sovesudil hydrochloride (PHP-201 hydrochloride; AMA0076 hydrochloride) V76489 Sovesudil hydrochloride (PHP-201 hydrochloride; AMA0076 hydrochloride) 2984963-50-8 Sovesudil (PHP-201) HCl is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor (antagonist) with IC50s of 3.7 and 2.3 nM for ROCK I and ROCK II, respectively.
SR-3677 V2951 SR-3677 1072959-67-1 SR-3677 (SR3677) is a potent and selective Rho-kinase/ROCK2 inhibitor with anticancer activity.
奈舒地尔甲磺酸盐 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.
甲磺酸贝舒地尔 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).
维罗舒地尔 V20464 Verosudil 1414854-42-4 Verosudil (AR-11324; AR 11324; AR11324) is a novel and potent Rho kinase inhibitorwith anti-hypertensive activity.
羟基法舒地尔 V2734 Hydroxyfasudil (HA-1100) 105628-72-6 Hydroxyfasudil (also called HA1100 HCl), a metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.
Contact Us