Search Result
Results for "
ROCK2 inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-10071
-
Y-27632
Maximum Cited Publications
533 Publications Verification
|
ROCK
NADPH Oxidase
mTOR
Reactive Oxygen Species (ROS)
NF-κB
Apoptosis
Akt
Autophagy
PAK
Ras
|
Cancer
|
|
Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade .
|
-
-
- HY-15307
-
|
KD025; SLx-2119
|
ROCK
|
Inflammation/Immunology
Cancer
|
|
Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
|
-
-
- HY-15392
-
|
|
ROCK
|
Cardiovascular Disease
|
|
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 .
|
-
-
- HY-10341
-
|
HA-1077 Hydrochloride; AT-877 Hydrochloride
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
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 .
|
-
-
- HY-103045
-
CMPD101
4 Publications Verification
|
ROCK
PKC
G Protein-coupled Receptor Kinase (GRK)
|
Cardiovascular Disease
|
|
CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
|
-
-
- HY-15556
-
|
GSK 269962
|
ROCK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-10341A
-
|
HA-1077; AT877
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
|
Cancer
|
|
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 .
|
-
-
- HY-148808
-
|
RXC007
|
ROCK
|
Cancer
|
|
Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma .
|
-
-
- HY-15307A
-
|
KD025 mesylate; SLx-2119 mesylate
|
ROCK
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-15720A
-
|
|
ROCK
|
Neurological Disease
|
|
H-1152 dihydrochloride is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
|
-
-
- HY-15685
-
-
-
- HY-15755
-
|
|
ROCK
|
Cancer
|
|
RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 values of 14.5 nM and 6.2 nM, respectively.
|
-
-
- HY-10319
-
BAY-549
4 Publications Verification
ROCK-IN-2; Azaindole 1; TC-S 7001
|
ROCK
|
Cardiovascular Disease
|
|
BAY-549 (Azaindole 1), a chemical probe, 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 .
|
-
-
- HY-119937
-
|
|
ROCK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
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 .
|
-
-
- HY-15687A
-
|
|
ROCK
|
Metabolic Disease
|
|
SAR407899 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 rat ROCK-2, respectively. SAR407899 shows stable inhibition of migrasome formation.
|
-
-
- HY-162596
-
|
BA-1049 free base
|
ROCK
|
Neurological Disease
|
|
NRL-1049 (BA-1049 (free base)) is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations .
|
-
-
- HY-108518
-
|
|
ROCK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
SB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases .
|
-
-
- HY-13911
-
-
-
- HY-15720
-
H-1152
4 Publications Verification
|
ROCK
|
Neurological Disease
|
|
H-1152 is a membrane-permeable and selective ROCK inhibitor, with a Ki value of 1.6 nM, and an IC50 value of 12 nM for ROCK2.
|
-
-
- HY-103620
-
|
|
ROCK
|
Inflammation/Immunology
Cancer
|
|
ROCK2-IN-2 (Example 2) is a ROCK2 inhibitor that can be used for the study of multiple medical disorders, such as fibrosis, inflammatory disorders, autoimmune disorders, and cardiovascular disorders .
|
-
-
- HY-13911A
-
-
-
- HY-12437
-
|
|
ROCK
|
Cancer
|
|
BDP5290 is a 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.
|
-
-
- HY-15556A
-
|
GSK 269962 hydrochloride
|
ROCK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-100270
-
|
|
ROCK
|
Cancer
|
|
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 .
|
-
-
- HY-16758
-
|
AR-12286
|
ROCK
|
Neurological Disease
|
|
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 .
|
-
-
- HY-10341C
-
|
HA-1077 dihydrochloride; AT-877 dihydrochloride
|
Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
|
Cancer
|
|
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 .
|
-
-
- HY-12659
-
LX7101
3 Publications Verification
|
LIM Kinase (LIMK)
ROCK
PKA
|
Endocrinology
|
|
LX7101 is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 has the potential for ocular hypertension and associated glaucoma research .
|
-
-
- HY-15687
-
|
|
ROCK
|
Metabolic Disease
|
|
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 rat ROCK-2, respectively.
|
-
-
- HY-149266
-
THK01
1 Publications Verification
|
ROCK
|
Cancer
|
|
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 .
|
-
-
- HY-150640
-
-
-
- HY-15392A
-
|
|
ROCK
|
Cardiovascular Disease
|
|
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 .
|
-
-
- HY-178821
-
|
|
ROCK
TGF-beta/Smad
STAT
|
Inflammation/Immunology
|
|
ROCK2-IN-12 (Compound A25) is a selective ROCK2 inhibitor with an IC50 of 7.0 nM for ROCK2 over ROCK1. ROCK2-IN-12 has potent antifibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrotic progression in Bleomycin (HY-108345)-induced pulmonary fibrosis (PF) mouse models. ROCK2-IN-12 can be used for lung diseases like pulmonary fibrosis research .
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-
-
- HY-156592A
-
|
|
ROCK
|
Inflammation/Immunology
|
|
ROCK2-IN-6 hydrochloride (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research .
|
-
-
- HY-126432
-
|
BA-1049
|
ROCK
|
Neurological Disease
|
|
NRL-1049 dihydrochloride (BA-1049) is a selective and orally active rho-associated protein kinase 2 (ROCK2) inhibitor with an IC50 of 0.59 μM. NRL-1049 dihydrochloride shows selectivity for ROCK2 is 44 times that of ROCK1 (IC50 = 26 μM). NRL-1049 dihydrochloride can preserve the blood-brain barrier after acute injury .
|
-
-
- HY-116420
-
|
|
ROCK
|
Neurological Disease
|
|
ROCK2-IN-8 (Compound 1) is an orally active ROCK2 inhibitor, with an IC50 of 7.2 nM. ROCK2-IN-8 can be used for the research of aqueous humor outflow in porcine eyes and myosin light chain phosphorylation .
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-
-
- HY-110339
-
|
|
ROCK
Apoptosis
|
Cancer
|
|
RKI 1447 dihydrochloride is a potent and selective ROCK inhibitor with IC50s of 14.5 and 6.2 nM for ROCK1 and ROCK2, respectively . RKI 1447 dihydrochloride suppresses colorectal carcinoma cell growth and promotes apoptosis .
|
-
-
- HY-178013
-
|
|
ROCK
|
Inflammation/Immunology
|
|
ROCK2-IN-11 (Compound A20) is a selective ROCK2 inhibitor with an IC50 of 0.18 μM for ROCK2 over ROCK1. ROCK2-IN-11 can be used for idiopathic pulmonary fibrosis and cGVHD research .
|
-
-
- HY-10071A
-
|
|
ROCK
NF-κB
Apoptosis
Autophagy
Akt
mTOR
NADPH Oxidase
Reactive Oxygen Species (ROS)
PAK
Ras
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Y-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade .
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-
-
- HY-15685A
-
|
K-115 free base
|
ROCK
|
Neurological Disease
|
|
Ripasudil free base (K-115 free base) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
|
-
-
- HY-126275
-
|
|
ROCK
|
Cancer
|
|
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 .
|
-
-
- HY-175843
-
|
|
ROCK
STAT
|
Cancer
|
|
ROCK2-IN-10 is a potent and selective ROCK2 inhibitor (IC50 = 0.020 μM) with 41-fold selectivity over isoform ROCK1. ROCK2-IN-10 inhibits metastasis by disrupting the cytoskeleton, independent of proliferative suppression. ROCK2-IN-10 shows superior inhibitory potency against cancer cell metastasis, which closely related to the suppression of STAT3 phosphorylation. ROCK2-IN-10 can be used for breast cancer metastasis research .
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-
-
- HY-15307AR
-
|
KD025 mesylate (Standard); SLx-2119 mesylate (Standard)
|
ROCK
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Belumosudil (mesylate) (Standard) is the analytical standard of Belumosudil (mesylate). This product is intended for research and analytical applications. 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 .
|
-
-
- HY-15307R
-
|
KD025 (Standard); SLx-2119 (Standard)
|
ROCK
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Belumosudil (Standard) is the analytical standard of Belumosudil. This product is intended for research and analytical applications. Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties .
|
-
-
- HY-U00351
-
-
-
- HY-149700
-
|
|
ROCK
MMP
STAT
|
Others
|
|
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model .
|
-
-
- HY-162798
-
|
|
ROCK
|
Cancer
|
|
ROCK2-IN-9 (compound 7u) is a selective ROCK2 inhibitor (IC50=36.8 nM) with anticancer activity. ROCK2-IN-9 inhibits cancer cell migration and invasion by regulating multiple cellular activities of the actin cytoskeleton. ROCK2-IN-9 can be used in breast cancer research .
|
-
-
- HY-15685R
-
|
K-115 (Standard)
|
ROCK
Reference Standards
|
Cardiovascular Disease
Neurological Disease
|
|
Ripasudil (Standard) is the analytical standard of Ripasudil. This product is intended for research and analytical applications. Ripasudil (K-115) is a specific inhibitor of ROCK, with IC50s of 19 and 51 nM for ROCK2 and ROCK1, respectively.
|
-
-
- HY-10833
-
|
|
ROCK
|
Cardiovascular Disease
|
|
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 .
|
-
-
- HY-122011
-
|
|
ROCK
SGK
PKA
PKC
|
Inflammation/Immunology
|
|
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 .
|
-
-
- HY-103045A
-
-
- HY-164809
-
|
|
ROCK
|
Metabolic Disease
|
|
KD025m1 is a novel selective ROCK2 inhibitor. KD025m1 has good anti obesity, improved insulin sensitivity, and blood glucose control effects. KD025m1 can be used to study metabolic diseases such as diabetes and obesity .
|
-
- HY-107209
-
|
|
ROCK
|
Cancer
|
|
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 .
|
-
- HY-10341R
-
|
HA-1077 Hydrochloride (Standard); AT-877 Hydrochloride (Standard)
|
Reference Standards
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
|
Cancer
|
|
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 .
|
-
- HY-156592
-
|
|
ROCK
|
Inflammation/Immunology
|
|
ROCK2-IN-6 (Comp A) is a selective ROCK2 inhibitor, can be used for ROCK mediated diseases, autoimmune diseases and inflammation research .
|
-
- HY-145294
-
|
|
ROCK
|
Neurological Disease
|
|
ROCK2-IN-5 (compound 1d) is a hybrid compound containing structural fragments of the Rho kinase inhibitor fasudil and the NRF2 inducers caffeic and ferulic acids. ROCK2-IN-5 has good multitarget profile and good tolerability. ROCK2-IN-5 has the potential for thr research of Amyotrophic lateral sclerosis (ALS) with a SOD1 mutation .
|
-
- HY-15307S
-
|
KD025-d7; SLx-2119-d7
|
Isotope-Labeled Compounds
ROCK
|
Inflammation/Immunology
Cancer
|
|
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 .
|
-
- HY-113641
-
-
- HY-W295201
-
|
|
ROCK
|
Cancer
|
|
ROCK-IN-11 (example 94) is a potent inhibitor of ROCK1 and ROCK2, with the IC50 of ≤ 5μM. ROCK-IN-11 plays an important role in cancer research .
|
-
- HY-100460
-
|
|
ROCK
|
Cancer
|
|
BIPM is a potent ROCK2 inhibitor. BIPM leads to significant changes in neurite length, cell migration and actin stress fibers. BIPM plays an important role in anti-cancer metastasis .
|
-
- HY-13911AR
-
|
HA-1100 hydrochloride (Standard); HA 1100 hydrochloride (Standard); HA1100 hydrochloride (Standard)
|
ROCK
Reference Standards
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Hydroxyfasudil (hydrochloride) (Standard) is the analytical standard of Hydroxyfasudil (hydrochloride). This product is intended for research and analytical applications. Hydroxyfasudil hydrochloride is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
|
-
- HY-13911R
-
-
- HY-16758A
-
|
AR-12286 hydrochloride
|
ROCK
|
Neurological Disease
|
|
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 .
|
-
- HY-N15301
-
|
|
ROCK
Myosin
|
Others
|
|
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 .
|
-
- HY-10341B
-
|
HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
|
ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
|
Cancer
|
|
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 .
|
-
- HY-10341D
-
|
HA-1077 mesylate; AT-877 mesylate
|
ROCK
Calcium Channel
Autophagy
PKA
PKC
|
Cancer
|
|
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 .
|
-
- HY-12659B
-
|
|
LIM Kinase (LIMK)
ROCK
PKA
|
Endocrinology
|
|
LX7101 monohydrochloride is a potent LIM-kinase, ROCK and PKA inhibitor with IC50s of 24 nM, 1.6 nM, 10 nM and <1 nM for LIMK1, LIMK2, ROCK2 and PKA, respectively. LX7101 monohydrochloride proves significantly selective for LIMK2 with IC50 values of 4.3 nM and 32 nM for LIMK2 and LIMK1 at 2 μM ATP, respectively. LX7101 monohydrochloride has the potential for ocular hypertension and associated glaucoma research .
|
-
- HY-172177
-
|
|
Apoptosis
HDAC
ROCK
|
Cancer
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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) .
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- HY-103620R
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Reference Standards
ROCK
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Inflammation/Immunology
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ROCK2-IN-2 (Standard) is the analytical standard of ROCK2-IN-2 (HY-103620). This product is intended for research and analytical applications. ROCK2-IN-2 is a selective ROCK2 inhibitor extracted from patent US20180093978A1, Compound A-30, has an IC50 of <1 μM.
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- HY-179498
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FOXO
PTEN
ROCK
Epigenetic Reader Domain
PI3K
Akt
Apoptosis
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Cancer
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ROCK2-IN-13 is a selective ROCK2 inhibitor. ROCK2-IN-13 reduces nuclear expression by disrupting the interaction of ROCK2 with transcriptional co activators p300> and PGC 1α, repressing oncogenic transcription. ROCK2-IN-13 activates FOXO1 driven PTEN expression, leading to suppression of the PI3K/Akt pathway, induction of G2/M cell cycle arrest, and promotion of apoptosis. ROCK2-IN-13 ablates the nuclear transcriptional function of ROCK2 that sustains oncogenic signaling and restores the tumor suppressive PTEN/FOXO1 axis. ROCK2-IN-13 can be used for prostate cancer reseach .
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- HY-181576
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ROCK
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Inflammation/Immunology
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ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 can be used for research on atopic dermatitis .
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- HY-181583
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ROCK
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Cancer
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LASSBio-2389 is a selective ROCK2 inhibitor with an IC50 of 0.051 μM and an IC50 of 1.143 μM against ROCK1. LASSBio-2389 reduces the viability of MDA-MB-231 cells and inhibits cell migration. LASSBio-2389 is applicable to the research of triple-negative breast cancer .
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- HY-181582
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ROCK
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Cancer
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LASSBio-2382 is a dual ROCK1/ROCK2 inhibitor with ROCK1 IC50 of 0.005 μM and ROCK2 IC50 of 0.003 μM. LASSBio-2382 inhibits viability and migration of cancer cells. LASSBio-2382 can be used for the research of triple-negative breast cancer .
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- HY-162596A
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(Rac)-BA-1049
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ROCK
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Neurological Disease
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(Rac)-NRL-1049 is the racemic mixture of NRL-1049 (BA-1049 (free base)) (HY-162596). NRL-1049 is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations .
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- HY-10319R
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ROCK-IN-2 (Standard); Azaindole 1 (Standard); TC-S 7001 (Standard)
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Reference Standards
ROCK
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Cardiovascular Disease
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BAY-549 (Standard) is the analytical standard of BAY-549 (HY-10319). This product is intended for research and analytical applications. BAY-549 (Azaindole 1), a chemical probe, 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 .
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- HY-100270R
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ROCK
Reference Standards
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Cancer
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Rho-Kinase-IN-1 (Standard) is the analytical standard of Rho-Kinase-IN-1 (HY-100270). This product is intended for research and analytical applications. 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 .
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- HY-103045R
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ROCK
PKC
G Protein-coupled Receptor Kinase (GRK)
Reference Standards
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Cardiovascular Disease
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CMPD101 (Standard) is the analytical standard of CMPD101 (HY-103045). This product is intended for research and analytical applications. CMPD101 is a potent, highly selective and membrane-permeable small-molecule inhibitor of GRK2/3 with IC50 of 18 nM and 5.4 nM, respectively. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively. CMPD101 can be used for the study of heart failure .
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- HY-108518R
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Reference Standards
ROCK
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Cardiovascular Disease
Inflammation/Immunology
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SB-772077B dihydrochloride (Standard) is the analytical standard of SB-772077B (dihydrochloride) (HY-108518). This product is intended for research and analytical applications. SB-772077B dihydrochloride is an orally active aminofuran-based Rho Kinase ((ROCK)) inhibitor with IC50 values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytoKines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases .
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- HY-10071R
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Reference Standards
mTOR
Ras
ROCK
NADPH Oxidase
NF-κB
Reactive Oxygen Species (ROS)
Akt
Apoptosis
Autophagy
PAK
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Cancer
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Y-27632 (Standard) is the analytical standard of Y-27632 (HY-10071). This product is intended for research and analytical applications. Y-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N15301
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Microorganisms
Ketones, Aldehydes, Acids
Source Classification
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ROCK
Myosin
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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 .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-15307S
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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 .
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