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Results for "

Rho Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ROCK (22) Adrenergic Receptor (1) Apoptosis (4) Aurora Kinase (1) CaMK (1) Deubiquitinase (3) PKA (2) PKC (1) Ras (14) SGK (1)
By Research Areas:	Cancer (20) Cardiovascular Disease (2) Inflammation/Immunology (4) Metabolic Disease (3) Neurological Disease (10)

Inhibitors & Agonists

Peptides

Targets Recommended: ROCK

Cat. No.	Product Name	Target	Research Areas

HY-12649

Y16 4 Publications Verification	Ras	Cancer
Y16 is a specific inhibitor of *Leukemia-associated Rho* guanine nucleotide exchange factor (LARG) with a K_d value of 76 nM. Y16 is active in blocking the interaction of LARG** and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.

HY-150640

Rho-Kinase-IN-2	ROCK	Neurological Disease
Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC₅₀=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.

HY-100270

Rho-Kinase-IN-1	ROCK	Cancer
Rho-Kinase-IN-1 is a Rho kinase (ROCK) inhibitor (K_i values of 30.5 and 3.9 nM for ROCK1 and ROCK2, respectively) extracted from US20090325960A1, compound 1.008.

HY-118151

Rho-Kinase-IN-3	ROCK	Neurological Disease
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.

HY-126913

Rhodblock 6

ROCK Cancer

Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization.
HY-148808

Zelasudil

RXC007
ROCK Others

Zelasudil is a Rho-associated (ROCK) kinase inhibitor. Zelasudil has a ROCK2 binding affinity.

Rhodblock 6	ROCK	Cancer
Rhodblock 6 is a Rho kinase (ROCK) inhibitor that inhibits phospho-MRLC (myosin regulatory light chain) localization.

Zelasudil RXC007	ROCK	Others
Zelasudil is a Rho-associated (ROCK) kinase inhibitor. Zelasudil has a ROCK2 binding affinity.

HY-12798A

Netarsudil dimesylate AR-13324 dimesylate	ROCK	Others
Netarsudil mesylate (AR-13324 mesylate) is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes.

HY-P5158

Conopeptide rho-TIA	Adrenergic Receptor	Others
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α_1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α_1A-Adrenergic Receptor and *α_1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α₁-Adrenergic Receptor* subtype-selective drugs**.

HY-130011

CCG-232964

Ras ROCK Cancer Neurological Disease

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

CCG-232964	Ras ROCK	Cancer Neurological Disease
CCG-232964 is an orally active inhibitor of *Rho/MRTF/SRF. CCG-232964 inhibits* LPA-induced CTGF gene expression.

HY-12798B

Netarsudil hydrochloride AR-13324 hydrochloride	ROCK	Neurological Disease
Netarsudil hydrochloride (AR-13324 hydrochloride) is a Rho-associated protein kinas (ROCK) and norepinephrine transporter (NET) inhibitor. Netarsudil hydrochloride has effective in intraocular pressure (IOP) reduction.

HY-108518

SB-772077B dihydrochloride	ROCK	Cardiovascular Disease
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.

HY-117149

MLS000532223	Ras	Cancer
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC₅₀ values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases.

HY-17543

ML-323 5+ Cited Publications	Deubiquitinase	Cancer
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC₅₀ of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (K_i) is 68 nM.

HY-112362

3-(4-Pyridyl)indole Rockout; 3-(4-Pyridinyl)-1H-indole; Rho Kinase Inhibitor III, Rockout	ROCK	Inflammation/Immunology
3-(4-Pyridyl)indole (Rockout) is a Rho-kinase (ROCK) inhibitor, with an IC₅₀ of 25 μM. 3-(4-Pyridyl)indole can inhibit blebbing and cause dissolution of actin stress fibers in a wound healing assay.

HY-122011

PF-4950834	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-12875

BQU57	Ras	Cancer
BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA. The IC50 for BQU57 of 2.0 μM in H2122 and 1.3 μM in H358.

HY-18990

GSK180736A 4 Publications Verification	ROCK	Cardiovascular Disease
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.

HY-118837

WF-536	ROCK	Cancer
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-10583

Y-27632 dihydrochloride Maximum Cited Publications 194 Publications Verification	ROCK	Cancer Neurological Disease
Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I K_i=220 nM; ROCK-II K_i=300 nM). Y-27632 dihydrochloride shows antiepileptic effects.

HY-111432

CCG-232601	Ras	Others
CCG-232601 (compound 8f) is a potent and orally active *Rho/MRTF/SRF* transcriptional pathway inhibitor. CCG-232601 inhibits the development of Bleomycin-induced dermal fibrosis in mice. CCG-232601 has the potential for the research of antifibrotic for systemic scleroderma.

HY-139170

CAY10746	ROCK	Metabolic Disease
CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC₅₀ values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR).

HY-121750

CCG-222740	Ras ROCK	Cancer
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.

HY-109191A

Sovesudil hydrochloride PHP-201 hydrochloride; AMA0076 hydrochloride	ROCK	Neurological Disease
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.

HY-109191

Sovesudil PHP-201; AMA0076	ROCK	Others
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.

HY-13991

CCG-1423 5+ Cited Publications	Ras Apoptosis	Cancer
CCG-1423 is an inhibitor of *Rho/MRTF/SRF* pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes.

HY-111458

GSK2643943A 3 Publications Verification	Deubiquitinase	Cancer
GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC₅₀ of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .

HY-16758

Verosudil AR-12286	ROCK	Neurological Disease
Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with K_is of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork.

HY-108361

CCG-203971	Ras	Inflammation/Immunology Cancer
CCG-203971 is a second-generation *Rho/MRTF/SRF* pathway inhibitor. CCG-203971 potently targets RhoA/C-activated SRE-luciferase (IC₅₀ =6.4 μM). CCG-203971 inhibits PC-3 cell migration with an IC₅₀ of 4.2 μM. Potential anti-metastasis Agent.

HY-12646A

Rhosin	Ras Apoptosis	Cancer
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.

HY-15720B

Glycyl H-1152 hydrochloride	ROCK Aurora Kinase CaMK	Neurological Disease
Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC₅₀s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.

HY-12646

Rhosin hydrochloride 20+ Cited Publications	Ras Apoptosis	Cancer
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a K_d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.

HY-134817

USP7-IN-8	Deubiquitinase	Cancer
USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC₅₀ of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.

HY-10583G

Y-27632 dihydrochloride	ROCK	Cancer Neurological Disease
Y-27632 dihydrochloride (GMP) is the GMP level of Y-27632 dihydrochloride (HY-10583). GMP guidelines are used to produce Y-27632 dihydrochloride (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor with antiepileptic effect.

HY-145294

ROCK2-IN-5	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-137638

Sp-5,6-DCl-cBIMPS	PKA	Metabolic Disease
Sp-5,6-DCl-cBIMPS is a potent and specific cAMP-dependent protein kinases (cAMP-PK) activator. Sp-5,6-DCl-cBIMPS stimulates insulin release. Sp-5,6-DCl-cBIMPS inhibits U46619-induced activation of Rho, Gq and G12/G13 in platelets.

HY-13991A

(S)-CCG-1423	Ras Others	Cancer Metabolic Disease
(S)-CCG-1423 is an inhibitor of *Rho* signaling that blocks the nuclear import of MRTF-A. (S)-CCG-1423 reduces the nuclear accumulation of MRTF-A and improves glucose uptake and tolerance in insulin-resistance mice in vivo. (S)-CCG-1423 exhibits higher inhibition activity than the SR- and the R-isomers of CCG-1423 (HY-13991). (S)-CCG-1423 can be used for the research of cancer and diabetes.

HY-12755

ML141 15+ Cited Publications CID-2950007	Ras Apoptosis	Cancer
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC₅₀s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.

HY-152095

PPI-GIT1/β-Pix interaction-IN-1	Ras	Cancer
PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a K_D value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer.

HY-115376

Z62954982 ZINC08010136	Ras	Inflammation/Immunology
Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC₅₀=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC₅₀=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).