Search Result
Results for "
RhoA Inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-12646A
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Rhosin
Maximum Cited Publications
34 Publications Verification
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Ras
Apoptosis
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Cancer
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Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd 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 .
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- HY-12646
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Ras
Apoptosis
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Cancer
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Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd 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 .
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- HY-145915A
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Ras
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Cancer
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(E/Z)-ZINC09659342 is an inhibitor of Lbc-RhoA interaction .
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- HY-15477A
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Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors .
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- HY-168596
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ROCK
Apoptosis
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Cancer
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RhoA-ROCK-IN-1 (Compound b19) is an inhibitor of RhoA/ROCK. RhoA-ROCK-IN-1 can significantly inhibit cell proliferation, migration, and invasion, while promoting cell apoptosis. RhoA-ROCK-IN-1 demonstrates remarkable anticancer activity by inhibiting the RhoA/ROCK pathway .
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- HY-121667
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ROCK
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Cancer
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Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation .
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- HY-176267
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Ras
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Cardiovascular Disease
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AH001 is a orally active RhoA inhibitor, which binds a cryptic pocket proximate to GDP within RhoA with a KD of 73.16 nM. AH001 interacts with GDP, stabilizing RhoA’s interaction with its endogenous inhibitor, RhoGDIα. AH001 reduces the downstream MRTFA nuclear translocation and downregulates fibrosis/hypertrophy proteins. AH001 mitigates myocardial remodeling in multiple HF animal models, and in the 3D myocardial tissue model. AH001 exerts its cardioprotective effects through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signaling.
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- HY-145915
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Ras
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Cancer
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ZINC09659342 (compound 13) is an inhibitor of Lbc-RhoA interaction with an IC50 of 3.6 μΜ .
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- HY-158652
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Ras
Akt
PI3K
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Cancer
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(R)-CCG-1423 is an inhibitor of RhoA. (R)-CCG-1423 inhibits downstream of Rho and shows specificity for SRE .
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- HY-N14739
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Ras
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Cancer
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Dykellic acid is a RhoA inhibitor. Dykellic acid can inhibit the migration and motility of B16 cells and the tube formation of HUVECs. Dykellic acid is promising for research of cancers .
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- HY-15477
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Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors .
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- HY-172917
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Ras
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Cancer
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Rho GTPase inhibitor 1 (compound 7) is a potent Rho GTPase inhibitor. Rho GTPase inhibitor 1 exhibits high affinity on Cdc42, Rac1 and RhoA with KDs of 151, 352, and 232 μM, respectively. Rho GTPase inhibitor 1 reduces cell migration on glioma cell line .
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- HY-109523
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HMG-CoA Reductase (HMGCR)
Ferroptosis
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Cardiovascular Disease
Cancer
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Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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- HY-108361
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Ras
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Inflammation/Immunology
Cancer
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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 .
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- HY-129458
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HMG-CoA Reductase (HMGCR)
Ferroptosis
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Cardiovascular Disease
Cancer
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Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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- HY-P990805
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HSP
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Metabolic Disease
Cancer
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Anti-Human/Mouse GRP78 Antibody (C38) is a kind of mouse IgG2b antibody inhibitor, targeting to GRP78. Anti-Human/Mouse GRP78 Antibody (C38) inhibits RhoA, ROCK and AKT activation. Anti-Human/Mouse GRP78 Antibody (C38) can be used for the researches of cancer and metabolic disease, such as melanoma and diabetes .
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- HY-12649
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Ras
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Cancer
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Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd 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 .
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- HY-113849
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MLS000573151
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Ras
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Inflammation/Immunology
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MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42 .
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- HY-109523S
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Ferroptosis
HMG-CoA Reductase (HMGCR)
Isotope-Labeled Compounds
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Cardiovascular Disease
Cancer
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Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
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- HY-139061
-
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LPL Receptor
ROCK
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Cancer
|
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Palmitoyl 3-carbacyclic phosphatidic acid (HY-139061) is a palmitoylated Carba-like cyclophosphatidic acid and an analog of lysophosphatidic acid (LPA). Palmitoyl 3-carbacyclic phosphatidic acid has different functions from LPA and can inhibit the activation of RhoA and inhibit the migration of melanoma cells. Palmitoyl 3-carbacyclic phosphatidic acid effectively inhibited experimental lung metastasis and reduced the number of tumor nodules in a B16-F0 xenograft mouse model .
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- HY-10341A
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HA-1077; AT877
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ROCK
Calcium Channel
Autophagy
PKA
PKC
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Cancer
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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 .
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- HY-10341
-
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HA-1077 Hydrochloride; AT-877 Hydrochloride
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ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
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Cancer
|
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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 .
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- HY-10341C
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HA-1077 dihydrochloride; AT-877 dihydrochloride
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Calcium Channel
ROCK
PKA
PKC
Autophagy
HIV
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Cancer
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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 .
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- HY-10341B
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HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
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ROCK
Calcium Channel
Autophagy
HIV
PKA
PKC
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Cancer
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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 .
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- HY-10341D
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HA-1077 mesylate; AT-877 mesylate
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ROCK
Calcium Channel
Autophagy
PKA
PKC
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Cancer
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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 .
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- HY-P2325
-
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Biochemical Assay Reagents
ROCK
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Neurological Disease
Metabolic Disease
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Exoenzyme C3, clostridium botulinum, is a mono-ADP-ribosylating enzyme. Exoenzyme C3, clostridium botulinum specifically modifies RhoA, B, and C by transferring ADP-ribose to them, thereby inactivating these GTPases. Exoenzyme C3, clostridium botulinum can induce neuronal axonal and dendritic growth, inhibit macrophage migration, and regulate cytoskeletal dynamics. Exoenzyme C3, clostridium botulinum can be used in the research of spinal cord injury and diabetic painful neuropathy .
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- HY-10341R
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HA-1077 Hydrochloride (Standard); AT-877 Hydrochloride (Standard)
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Reference Standards
ROCK
Calcium Channel
Autophagy
PKA
PKC
HIV
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Cancer
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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 .
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- HY-115376
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ZINC08010136
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Ras
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Inflammation/Immunology
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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) .
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- HY-117548
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UNC1062
2 Publications Verification
|
TAM Receptor
Apoptosis
p38 MAPK
ERK
PI3K
Akt
JAK
STAT
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Cardiovascular Disease
Cancer
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UNC1062 is a highly selective tyrosine kinase (MERTK) inhibitor with an IC50 of 1.1 nM (Morrison Ki = 0.33 nM). UNC1062 exhibits good selectivity for the TAM family (TYRO3 IC50 = 60 nM, AXL IC50 = 85 nM). UNC1062 exhibits significant anti-proliferative effects and induces apoptosis in various cancer models (such as melanoma, gastric cancer, and acute myeloid leukemia). UNC1062 inhibits multiple pathways, including MAPK/ERK, PI3K/AKT and JAK/STAT and affects the motility of head and neck squamous cell carcinoma (HNSCC) cells through the RhoA signaling pathway. UNC1062 inhibits macrophage efferocytosis, and it suitable for research on atherosclerosis .
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- HY-I0400
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NANA; Lactaminic acid
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Tyrosinase
Ras
Influenza Virus
Endogenous Metabolite
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
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- HY-135457
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JMS-053
3 Publications Verification
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Phosphatase
STAT
Ras
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Cancer
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JMS-053 is an efficient and reversible PTP4A3 inhibitor, with an IC50 value of 18 nM.
JMS-053 demonstrates broad PTP4A inhibitory activity with IC50s of 50 nM and 53 nM for PTP4A1 and PTP4A2, respectively. JMS-053 exhibits IC50 values of 92.6 nM and 207.6 nM for CDC25B and DUSP3, respectively. JMS-053 can effectively inhibit the activity of PTP4A3, inhibit tumor cell proliferation and migration through multiple mechanisms such as interfering with RhoA and STAT3/p38 signaling pathway. JMS-053 can be used for the study of cancers such as ovarian cancer, breast cancer and colon cancer .
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- HY-I0400R
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NANA (Standard); Lactaminic acid (Standard)
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Reference Standards
Tyrosinase
Ras
Influenza Virus
Endogenous Metabolite
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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N-Acetylneuraminic acid (Standard) is the analytical standard of N-Acetylneuraminic acid. This product is intended for research and analytical applications. N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
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- HY-105284R
-
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CP-70429 (Standard)
|
Beta-lactamase
Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
N-Acetylneuraminic acid (Standard) is the analytical standard of N-Acetylneuraminic acid. This product is intended for research and analytical applications. N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
|
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990805
-
|
|
HSP
|
Metabolic Disease
Cancer
|
|
Anti-Human/Mouse GRP78 Antibody (C38) is a kind of mouse IgG2b antibody inhibitor, targeting to GRP78. Anti-Human/Mouse GRP78 Antibody (C38) inhibits RhoA, ROCK and AKT activation. Anti-Human/Mouse GRP78 Antibody (C38) can be used for the researches of cancer and metabolic disease, such as melanoma and diabetes .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-I0400
-
-
-
- HY-I0400R
-
|
NANA (Standard); Lactaminic acid (Standard)
|
Microorganisms
Source classification
Endogenous metabolite
Saccharides
Monosaccharides
|
Reference Standards
Tyrosinase
Ras
Influenza Virus
Endogenous Metabolite
|
|
N-Acetylneuraminic acid (Standard) is the analytical standard of N-Acetylneuraminic acid. This product is intended for research and analytical applications. N-Acetylneuraminic acid (NANA; Lactaminic acid), a nonphenolic structure, is the predominant form of sialic from Collocalia esculenta. N-Acetylneuraminic acid plays a biological role in myocardial injury, melanoma and viral or bacterial infection. N-Acetylneuraminic acid inhibits melanogenesis by reducing tyrosinase activity and triggers myocardial injury in vitro and in vivo by activation of the Rho/Rho-associated signaling pathway through binding to RhoA and Cdc42. N-Acetylneuraminic acid may prevent high fat diet (HFD)-induced inflammation and oxidative stress, thereby prevents hyperlipidemia-associated inflammation and oxidative stress. N-Acetylneuraminic acid is promising for research in the field of melanoma, coronary artery, obesity-related diseases and hyperlipidemia .
|
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- HY-N14739
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-109523S
-
|
|
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Cerivastatin-d3 sodium is deuterated labeled Cerivastatin sodium (HY-109523). Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
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