rho gtpases

1A-116 is a specific inhibitor of Rac1 .

MLS000532223 is a selectiveRho family GTPases inhibitor(EC50 : 16 μM to 120 μM).

Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) activates signal-transducing G proteins involved in cellular processes such as proliferation, differentiation, and activation of intracellular kinase cascades. It regulates proliferation and apoptosis through the hydrolysis by small GTPases Ras and Rho, and plays a role in vesicle docking, fusion, and formation via Rab. Additionally, GTP serves as an energy-rich precursor for the biosynthesis of DNA and RNA.

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.

Guanosine triphosphate tritris (GTP tritris) serves as a crucial enhancer in myocyte differentiation, playing an essential role in regulating miRNA-muscle regulatory factors. It promotes the release of exosomes rich in guanine and guanine-derived molecules, and is considered an activation precursor for RNA synthesis. In mitochondrial functionality, GTP is involved in the entry of proteins into the matrix, which is vital for various regulatory pathways. It initiates peptide synthesis by facilitating the binding of formylmethionine-tRNA to the ribosome, and aids in polypeptide chain elongation. Additionally, GTP acts as a carrier for phosphates and pyrophosphates, channeling chemical energy into specific biosynthetic pathways. It activates signal transduction G proteins, regulates cellular processes such as proliferation and differentiation, and its hydrolysis by small GTPases (including Ras and Rho) is indispensable for both proliferation and apoptosis. Furthermore, the small GTPase Rab assists in vesicle docking, fusion, and formation. Beyond signal transduction, GTP is also an energy-rich precursor in the biosynthesis of DNA and RNA enzymes.

BAY 593 functions as an inhibitor of geranylgeranyltransferase-I (GGTase-I), effectively preventing the activation of Rho-GTPases and consequently inactivating YAP1/TAZ signaling pathways. It has been shown to inhibit tumor growth dose-dependently in xenograft mouse models, exhibiting IC50 values of 38.4 nM in MT-1080 cells and 564 nM in MDA-MB-231 cells, as well as in PXF 541 xenografts.

IMM-01 is a novel class of small-molecule agonists of the mammalian Diaphanous (mDia)-related formins, which act downstream of Rho GTPases to assemble actin filaments, and their organization with microfilaments to establish and maintain cell polarity during migration and asymmetric division. GTP-bound Rho activates mDia family members by disrupting the interaction between the DID and DAD autoregulatory domains, which releases the FH2 domain to modulate actin and microtubule dynamics[1].

PKN1/2-IN-1 is a potent and selective PKN2 inhibitor with 14-fold higher selectivity for PKN2 than PKN1, membrane permeability and anticancer potential.Protein kinase N proteins (PKN1, PKN2 and PKN3) are effectors of Rho GTPases and are critical for survival in several tumor cell lines including prostate and breast cancer.

Morelloflavone is a biflavonoid derived from Garcinia cambogia with anticancer property that inhibits tumor angiogenesis by targeting Rho GTPases and the extracellular signal-regulated kinase (ERK) signaling pathway. Fukugetin inhibits the cellular proliferation of a variety of cancer cell lines, such as Caspase-9, TNF -α, ER-α, , HER-2.

Rac GTPase fragment is a peptide with the sequence H2N-Val-Phe-Asp-Glu-Ala-Ile-Arg-Ala-Val-OH, MW= 1019.15. Rac is a subfamily of the Rho family of GTPases, small signaling G proteins (more specifically a GTPase).