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.

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

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.

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.

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].

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.

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

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.

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.

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

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.

RGS2–Galpha-q interaction-IN-1 (Compound AJ-3) is an inhibitor of the RGS2-Galpha-q interaction. It inhibits the growth of cancer cell lines that express RGS2 and has anti-cell migration properties.

CCG-4986 is the first small molecule RGS inhibitor reported that directly bound to an RGS protein.

CCG-2046 is a chemical inhibitor targeting RGS4, demonstrating an inhibition concentration (IC50) of 4.3 μM for the interaction between RGS4 and Gαo signal.

Myristoylated ARF6 (2-13) inhibits the MyD88–ARNO–ARF6 signaling axis by inactivating ARF6.

BMS-192364 is a bio-active chemical.

RGS10 modulator-1 (compound 15) is an effective regulator of RGS10. It significantly reverses IFNγ-induced expression of both RGS10 protein and mRNA, as well as COX-2 mRNA and iNOS expression triggered by IFNγ.