GTPase

Compound C108 is an inhibitor of GTPase-activating protein SH3 domain-binding protein 2 (G3BP2). Compound C108 can be used in studies about breast tumors and esophageal squamous cell carcinoma.

Anti-inflammatory agent 49 is a potent inhibitor of Drp1-Fis1 interaction, inhibits GTPase, and can be used in the study of diseases caused by mitochondrial dysfunction.

CID-4785700 is a potent pan-GTPase inhibitor that inhibits Rab7 and inhibits the fungal histone acetyltransferase Rtt109 that binds to Asf1 and Vps75, and can be used in the study of lupus.

NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.

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.

BQU57 selectively inhibits Ral over Ras or Rho and suppresses xenograft tumor growth.

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].

CCG-50014 is a potent and selective inhibitor of RGS4 with IC50 of 30 nM.

CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.

RBC10 inhibits the binding of Ral to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines.

CCG-63802 is a reversible inhibitor of the regulator of G-protein signaling (RGS) protein and has the greatest potency at RGS4.

QS11 is a GTPase activating protein of ADP-ribosylation factor 1 (ARFGAP1) inhibitor. Modulates ARF-GTP levels and synergizes with the Wnt β-catenin signaling pathway to upregulate β-catenin nuclear translocation. Also reduces in vitro migration of metastatic human breast cancer cells.

ML-097 (CID-2160985) is a universal activator of Ras-related GTPases.

CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins, dose-dependently inhibiting the TR-FRET signal between RGS4-AF488 and Tb-Gαo with an IC50 value of 1.9 μM.

Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) is a potent GTPase inhibitor that inhibits EGFR kinase with an IC50 of 560 μM.Tyrphostin 8 inhibits protein serine threonine calmodulin phosphatases (IC50=21 μM), enhances transferrin receptor-mediated transcytosis in Caco-2 cells, and increases the hypoglycemic effect of oral insulin-transferrin. hypoglycemic effect.

Exo-1 (Methyl 3-(4-fluorobenzoyl)-6-methyl-2-pyridinecarboxylate) is a synthetic compound that has been shown to affect the metabolism of various nutrients, as well as the regulation of various hormones. It has also been shown to have anti-inflammatory and anti-tumor effects.

Dynamin inhibitory peptide Acetate is a peptide with the sequence Gln-Val-Pro-Ser-Arg-Pro-Asn-Arg-Ala-Pro that inhibit the GTPase dynamin.

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.

Gancaonin I exhibits anti-BsFtsZ GTPase activities; it also shows significant inhibitory activity against B. subtilis, with a MIC value of 5 uM.