2. Signaling Pathways
  3. GPCR/G Protein
  4. Arf Family GTPase

Arf Family GTPase

ADP-ribosylation Factor (ARF) Family GTPase

ADP-ribosylation factor (Arf) GTPases are a subfamily of the Ras superfamily of small GTPases. In mammals, there are approximately 30 members of the ARF GTPases family, divided into "true ARFs" (6 types) and "ARF-like" (ARL) proteins (21 types), as well as other related proteins such as SARs. ARF GTPases play a crucial role in regulating membrane trafficking and organelle structure. They are activated and deactivated through GTP binding and hydrolysis, mediated by guanine nucleotide exchange factors (GEFs) and GTPase-activating proteins (GAPs). ARF GTPases regulate a variety of key cellular processes such as vesicle formation, protein sorting, lipid remodeling, and the dynamics of the cytoskeleton, thereby affecting secretion, endocytosis, and cell adhesion. Their activity involves interactions with a variety of effectors, including coat proteins, lipid-modifying enzymes, and scaffold proteins.
The aberrant expression or dysfunction of ARF GTPases is associated with various disease states, including neurodegenerative diseases, tumors, and immune system disorders. Specifically, the role of ARF GTPases in membrane remodeling and cell signaling makes them potential targets for research into these diseases[1].

Arf Family GTPase Related Products (10):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-112670
    Exo1
    		Modulator 99.77%
    Exo1 is a chemical inhibitor of the exocytic pathway.
    Exo1
  • HY-12762
    QS11
    		Inhibitor 99.10%
    QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
    QS11
  • HY-111549
    Bragsin1
    		Inhibitor 99.91%
    Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity.
    Bragsin1
  • HY-151461
    CHNQD-01255
    		Inhibitor
    CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy.
    CHNQD-01255
  • HY-173350
    Ran-IN-1
    		Inhibitor
    Ran-IN-1 (Compound M36) is an orally active and selective Ran GTPase inhibitor. Ran-IN-1 binds to the GDP-bound form of Ran (RanGDP) at the allosteric switch II pocket with high specificity, stabilizing the inactive state and reducing the active Ran-GTP population. Ran-IN-1 induces apoptosis and represses DNA repair pathways like HR and NHEJ in epithelial ovarian cancer (EOC) cells. Ran-IN-1 is promising for research of EOC, particularly high-grade serous carcinoma.
    Ran-IN-1
  • HY-173280
    Brefeldin A 4-O-nicotinate
    		Inhibitor
    Brefeldin A 4-O-nicotinate (CHNQD-01228) is a dual inhibitor of Arf1 and BMX proteins. The IC50 value for the proliferation of T24 cells is 0.22 μM. It can also dose-dependently inhibit the migration and colony formation of T24 cells, induce G1 phase arrest and trigger Apoptosis. Brefeldin A 4-O-nicotinate exerts its anti-cancer activity by targeting the BMX protein to inhibit the AKT/p-AKT and STAT3/p-STAT3 signaling pathways, as well as by inhibiting the Arf1 protein to eliminate bladder cancer stem cells and activate anti-tumor immunity. Brefeldin A 4-O-nicotinate can be used in the research related to bladder cancer.
    Brefeldin A 4-O-nicotinate
  • HY-175290
    Arf1-GEFs-IN-1
    		Inhibitor
    Arf1-GEFs-IN-1 is a potent and orally active ADP-ribosylation factor 1- guanine nucleotide exchange factors (Arf1-GEFs) inhibitor with an IC50 value of 40.85 μM against CT26 cells. Arf1-GEFs-IN-1 primarily mediates tumor regression by triggering anti-tumor immune responses, rather than through direct cytotoxicity. Arf1-GEFs-IN-1 effectively promotes CCL5 expression, demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 can be used for the study of colon cancer.
    Arf1-GEFs-IN-1
  • HY-P10179
    ARF6 (2-13)
    ARF6 (2-13) is a peptide with a sequence of GKVLSKIFGNKE. ARF6 (2-13) is an inhibitor of ARF6. ARF6 (2-13) can be used in the research of endotoxemia.
    ARF6 (2-13)
  • HY-173535
    TNP-β-L-GTP tetrasodium
    TNP-β-L-GTP (TNP-β-L-Guanosine 5'-triphosphate) tetrasodium is a fluorescent GTP mimetic that can be used to study the binding kinetics and affinity of GTP-binding proteins (such as G proteins and GTPases). TNP-β-L-GTP tetrasodium carries a TNP fluorophore, which changes fluorescence intensity upon protein binding, allowing for quantitative analysis.
    TNP-β-L-GTP tetrasodium
  • HY-P10178
    Myristoylated ARF6 (2-13)
    		Inhibitor
    Myristoylated ARF6 (2-13) blocks MyD88–ARNO–ARF6–signaling axis by deactivating ARF6.
    Myristoylated ARF6 (2-13)