ROCK Inhibitor

ROCK Inhibitors (167):

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-13300A

SR-3677 dihydrochloride	Inhibitor
SR-3677 dihydrochloride (compound 5) is a potent and selective ROCK-I and ROCK-II inhibitor with an IC₅₀ values of 56 nM and 3 nM.

HY-12798CR

AR-13503 (Standard)	Inhibitor
Fluanisone (Standard) is the analytical standard of Fluanisone. This product is intended for research and analytical applications. Fluanisone has potent sedative effect in vivo. Fluanisone can be used to study schizophrenia.

HY-123484

ROCK-IN-D1	Inhibitor
ROCK-IN-D1 serves as a highly effective and selective inhibitor of ROCK.

HY-145294

ROCK2-IN-5	Inhibitor
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-162596A

(Rac)-NRL-1049 dihydrochloride	Inhibitor
(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.

HY-130011

CCG-232964	Inhibitor
CCG-232964 is an orally active inhibitor of Rho/MRTF/SRF. CCG-232964 inhibits LPA-induced CTGF gene expression.

HY-W047432

5-Nitro-1H-indazole-3-carbonitrile	Inhibitor
5-Nitro-1H-indazole-3-carbonitrile (DL0805) is a Rho kinase(ROCK) inhibitor with an IC₅₀ of 6.67 μM for ROCK-I. 5-Nitro-1H-indazole-3-carbonitrile reduces Norepinephrine (HY-13715)-induced transient contraction and inhibits contraction induced by increasing external calcium in the endothelium-denuded rings of rat models. 5-Nitro-1H-indazole-3-carbonitrile has a vasorelaxant activity but high toxicity. 5-Nitro-1H-indazole-3-carbonitrile can be used for cardiovascular diseases, especially hypertension research.

HY-10071A

Y-27632 hydrochloride hydrate	Inhibitor	99.65%
Y-27632 hydrochloride hydrate is a ROCK inhibitor with K_i 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.

HY-181583

LASSBio-2389	Inhibitor
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.

HY-12880

HA-100 dihydrochloride	Inhibitor
HA-100 dihydrochloride is a potent protein kinase inhibitor, with IC₅₀s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. HA-100 dihydrochloride also used as a ROCK inhibitor.

HY-118837

WF-536	Inhibitor
WF-536 is an orally active inhibitor of Rho-associated coiled-coil-containing protein kinase (ROCK). WF-536 has tumor anti-metastatic activity. WF-536 can be used for the research of cancer.

HY-181576

ROCK2-IN-14	Inhibitor
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.

HY-W295201

ROCK-IN-11	Inhibitor
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-176133

ROCK-IN-12	Inhibitor
ROCK-IN-12 (compound R3) is a selective ROCK inhibitor. ROCK-IN-12 can be used in the study of glaucoma.

HY-153564

ROCK-IN-6	Inhibitor
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC₅₀ of 2.19 nM. ROCK-IN-6 is extracted from patent WO2021164351 A1, example 7, has the potential for glaucoma and retinal diseases research.

HY-175843

ROCK2-IN-10	Inhibitor
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.

HY-N12466

3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine	Inhibitor
3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine (Compound 7) is an inhibitor of protein kinases, with IC₅₀s of 0.092, 0.26, 0.77 μM for PKC-α, ROCK, ASK1. 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine shows potent cytotoxicity against PC-3 cancer cells with an IC₅₀ value of 0.16 μM.

HY-116238

ROCK-IN-D2	Inhibitor
ROCK-IN-D2 is a potent and selective ROCK inhibitor.

HY-N15301

Nocarnickelamide B	Inhibitor
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-151189

ROCK-IN-4	Inhibitor
ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. ROCK-IN-4 reversibly depolymerizes F-actin, and suppresses mitochondrial respiration in human trabecular meshwork (HTM) cells. ROCK-IN-4 can be used for glaucoma or ocular hypertension research.

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