rhoa

CCG-1423, a selective RhoA pathway inhibitor, suppresses SRF-mediated transcription.

RhoA-ROCK-IN-1 (Compound b19) is an inhibitor of the RhoA ROCK pathway. It significantly inhibits cell proliferation, migration, and invasion, while promoting cell apoptosis (apoptosis). RhoA-ROCK-IN-1 exhibits strong anticancer activities by inhibiting the RhoA ROCK pathway.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

YS-49 is an activator of PI3K Akt (a downstream target of RhoA).

AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM

NSC 23766 trihydrochloride (Rac1 Inhibitor) is an inhibitor of Rac GTPase targeting Rac activation by GEFs (IC50: ~50 μM); no inhibitory for the closely related targets, RhoA or Cdc42.

RBC8 is a specific GTPases RalA RalB inhibitor by inhibiting the binding of Ral to its effector RALBP1, no inhibition on the GTPases RhoA and Ras.

Narciclasine (Lycoricidinol), a natural product, modulates the Rho Rho-kinase LIM kinase cofilin signaling pathway, greatly increasing GTPase RhoA activity.

MLS-573151 is a selective inhibitor of GTPase Cdc42(EC50 of 2 μM). It 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.

(E Z)-ZINC09659342 is an inhibitor of Lbc-Rho A interaction.

YS-49 (monohydrate) is an activator of PI3K Akt (a downstream target of RhoA).

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Rhosin hydrochloride is a specific inhibitor of the RhoA subfamily Rho GTPases and inhibits the RhoA-GEF interaction. Rhosin hydrochloride can significantly induce cell apoptosis without affecting cell cycle progression. [1]

Rhosin is an effective and specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction (Kd: ~ 0.4 uM). Rhosin does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin causes cell apoptosis.

CCG-100602 inhibits RhoA C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells (IC50 :9.8 μM).

Scaff10-8 is an inhibitor of AKAP-Lbc-RhoA interaction that acts by promoting the translocation of aquaporin-2 to the plasma membrane of renal collecting duct principal cells.

CHS-111 is a benzyl indazole compound that inhibits superoxide anion (O(2)(-)) generation and reduces fMLP-stimulated PLD activity (IC(50) 3.9±1.2μM). It inhibits the interaction of PLD1 with ADP-ribosylation factor (Arf) 6 and Ras homology (Rho) A, and reduces the membrane recruitment of RhoA in fMLP-stimulated cells.

JK-122 is a novel inhibitor of RHOA.

Y16 is a G protein-coupled Rho GEFs inhibitor that synergizes with Rhosin G04 to inhibit LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling. Y16 is also a specific inhibitor of LARG with a Kd of 76 nM.

NSC 23766 is a Rac1 GTPase inhibitor that inhibits Rac1 activation by targeting guanine nucleotide exchange factors (GEFs), while it has no inhibitory effect on the closely related targets Cdc42 and RhoA, affecting the cell cycle and inhibiting cell proliferation in a dose-dependent manner. It also regulates endothelial NO synthase expression and endothelial function, and inhibits platelet aggregation and γ-secretase activity.NSC23766 competitively inhibits M2 muscarinic acetylcholine receptor (M2 mAChR)-induced Rac1 activation in neonatal rat cardiomyocytes.

CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50: 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. This compound also inhibits PC-3 cell migration (IC50: 4.2 μM), as determined by a scratch wound assay. CCG-203971(CCG203971) causes no cytotoxicity when evaluated by the WST-1 assay. It is well tolerated in normal mice up to doses of 100 mg kg given intraperitoneally over five days.

Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].

ZINC09659342 (compound 13) is an inhibitor of the Lbc-RhoA interaction with an IC50 value of 3.6 μM.

YS-49 (monohydrate) is an isoquinoline compound alkaloid that functions as a PI3K Akt activator, specifically targeting a downstream effect of RhoA, to mitigate the activation of RhoA PTEN in 3-methylcholanthrene-treated cells. It also prevents the angiotensin II (Ang II)-induced proliferation of vascular smooth muscle cells (VSMCs) by promoting the expression of heme oxygenase (HO)-1. Additionally, YS-49 exerts a significant positive inotropic effect by stimulating cardiac β-adrenoceptors, showcasing its multifaceted pharmacological activities [1] [2] [3].