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ROCK1-IN-1 is a ROCK1 inhibitor with a Ki value of 540 nM. ROCK1-IN-1 can be used for the research of hypertension, glaucoma and erectile dysfunction [1].
GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A hydrochloride has anti-inflammatory and vasodilatory activities [1].
GSK269962A (GSK 269962) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively. GSK269962A has anti-inflammatory and vasodilatory activities [1].
ROCK1 Human Pre-designed siRNA Set A contains three designed siRNAs for ROCK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Rock1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Rock1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
ROCK-IN-10 (compound 50) is a potent ROCK inhibitor with IC50 values of 6 nM and 4 nM for ROCK1 and ROCK2, respectively. ROCK-IN-10 shows >100-fold selectivity against other kinases [1].
BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC50s of 0.6 and 1.1 nM for human ROCK-1 and ROCK-2, respectively [1].
Nocarnickelamide B (Compound 2) is a linear peptide and ROCK1/2 inhibitor. Nocarnickelamide B exhibits dual inhibitory activity against ROCK1 and ROCK2 with IC50s of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B binds to the ATP-binding site. Nocarnickelamide B inhibits the activation of ROCK-regulated cytoskeletal contraction markers such as the myosin light chain. Nocarnickelamide B is potential for glaucoma reasearch [1].
Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties [1].
SB-772077B dihydrochloride is an aminofurazan-based Rho kinase (ROCK) inhibitor with IC50s of 5.6 nM and 6 nM toward ROCK1 and ROCK2, respevtively [1].
Rho-Kinase-IN-3 (compound 12) is a potent and selective Rho kinase (ROCK1) inhibitor with an IC50 value of 8 nM. Rho-Kinase-IN-3 can be used in research of hypertension [1].
Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (Ki values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008 [1].
RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively [1]. RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis .
PF-4950834 is a potent, selective, orally bioavailable, ATP-competitive rho kinase inhibitor with IC50 values of 8.35 nM and 33.12 nM against ROCK2 and ROCK1, respectively. PF-4950834 inhibits neutrophil migration [1].
GSK180736A is potent Rho-associated coiled-coil kinase 1(ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity [1].
GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 μM against hGWL FL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 μM, but only weakly affected PKA [1].
ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM. ROCK inhibitor-2 exhibits antitumor activity [1] .
Belumosudil-d7 (KD025-d7) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties [1].
CCG-224406 is a selective G protein-coupled receptor kinase 2 (GRK2) inhibitor with the IC50 values of 13 nM, greater than 700-fold selectivity over other GRK subfamilies, and no inhibition of ROCK1. CCG-224406 can be used for study of heart failure [1].
Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM [1] .
Chroman 1 dihydrochloride is a highly potent and selective ROCK inhibitor. Chroman 1 dihydrochloride is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM).
Chroman 1 dihydrochloride also has inhibitory activity against MRCK, with an IC50 of 150 nM [1] .
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer [1].
Verosudil (AR-12286) is a ROCK inhibitor. Verosudil has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil increases trabecular outflow capacity to reduce intraocular pressure. Verosudil is useful in the study of glaucoma and ocular hypertension [1] .
CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure [1].
DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer [1].
Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator [1] .
Verosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension [1] .
Fasudil (HA-1077; AT877) dihydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil dihydrochloride is also a potent Ca 2+ channel antagonist and vasodilator [1] .
Fasudil (HA-1077; AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca 2+ channel antagonist and vasodilator [1] .
Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca 2+ channel antagonist and vasodilator [1] .
Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil mesylate is also a potent Ca 2+ channel antagonist and vasodilator [1] .
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. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice [1].
Fasudil (Hydrochloride) (Standard) is the analytical standard of Fasudil (Hydrochloride). This product is intended for research and analytical applications. Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca 2+ channel antagonist and vasodilator [1] .
CCG258208 (GRK2-IN-1) hydrochloride is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 hydrochloride can be used in heart failure research [1].
CCG258208 (GRK2-IN-1) is a potent and selective GRK2 (G protein-coupled receptor kinase 2) inhibitor (IC50=30 nM) while maintaining 230-fold selectivity over GRK5 (IC50=7.09 μM) and more than 2500-fold selectivity over GRK1 (IC50=87.3 μM), PKA, and ROCK1. CCG258208 can be used in heart failure research [1].
ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC) [1].
AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells [1].
GSK-25 is a potent, selective and orally bioavailable ROCK1 inhibitor (IC50=7 nM). GSK-25 maintains good selectivity against a panel of 31 kinases (>100 fold), as well as RSK1 and p70S6K (RSK1: IC50=398 nM, p70S6K: IC50=1 μM). GSK-25 inhibits P450 profile (IC50s of 2.5, 5.2, 2.5 µM for CYP2C9, CYP2D6, CYP3A4, respectively) [1].
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits 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). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity [1].
Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia [1] .
RKI-1313 is a ROCK inhibitor with IC50s of 34, 8 µM for ROCK 1 and ROCK 2, respectively. RKI-1313 shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion or anchorage-independent growth [1].
Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia [1] .
Nocarnickelamide B (Compound 2) is a linear peptide and ROCK1/2 inhibitor. Nocarnickelamide B exhibits dual inhibitory activity against ROCK1 and ROCK2 with IC50s of 14.9 μM and 21.9 μM, respectively. Nocarnickelamide B binds to the ATP-binding site. Nocarnickelamide B inhibits the activation of ROCK-regulated cytoskeletal contraction markers such as the myosin light chain. Nocarnickelamide B is potential for glaucoma reasearch [1].
The ROCK1 protein is a key kinase that regulates the actin cytoskeleton, cell polarity, smooth muscle contraction, and multiple cellular functions. It controls stress fibers, focal adhesion formation, neurite retraction, and cell motility by phosphorylating substrates such as DAPK3, GFAP, LIMK1, LIMK2, MYL9/MLC2, TPPP, PFN1, and PPP1R12A. ROCK1 Protein, Human (sf9) is the recombinant human-derived ROCK1 protein, expressed by sf9 insect cells , with tag free.
The ROCK1 protein is a key kinase that regulates the actin cytoskeleton, cell polarity, smooth muscle contraction, and multiple cellular functions. It controls stress fibers, focal adhesion formation, neurite retraction, and cell motility by phosphorylating substrates such as DAPK3, GFAP, LIMK1, LIMK2, MYL9/MLC2, TPPP, PFN1, and PPP1R12A. ROCK1 Protein, Human (sf9, His) is the recombinant human-derived ROCK1 protein, expressed by sf9 insect cells , with N-8*His labeled tag.
Belumosudil-d7 (KD025-d7) is deuterium labeled Belumosudil. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties [1].
ROCK1 Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 158 kDa, targeting to ROCK1. It can be used for WB,ICC/IF,IHC-P,IP assays with tag free, in the background of Human, Mouse.
ROCK1 Human Pre-designed siRNA Set A contains three designed siRNAs for ROCK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Rock1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
Rock1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Rock1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
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