Arf Family GTPase Inhibitor

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.

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.

Ran-IN-1 is a specific inhibitor of Ran GTPase. Ran-IN-1 selectively induces cytotoxicity and apoptosis in aneuploid ovarian cancer cells and also inhibits DNA repair. Ran-IN-1 exhibits antitumor activity and is useful for research on tumors such as epithelial ovarian cancer.

ART5537 is a selective EXO1 inhibitor with a IC₅₀ of 3.4 nM and a K_d of 6.8 nM. ART5537 exerts cellular homologous recombination (HR) inhibition with EC₅₀ of 7.2 nM in HAP1 parental cells. ART5537 shows >200-fold selectivity over a panel of the wider nuclease superfamily. ART5537 exerts biological effects that are exclusively driven by EXO1 inhibition. ART5537 demonstrates sensitization to ionizing radiation and synergy with Olaparib (HY-10162). ART5537 can be used for research in breast cancer and colorectal adenocarcinoma.

IMP-2552 is a RAB27A/B inhibitor. IMP-2552 acts on the RAB27A/B effector protein-protein interaction, selectively modifying RAB27A/B-Cys123, but has no activity against RAB27A-Cys188. IMP-2552 can be used for the research of cancer.

CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy.

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.

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.

CHNQD-01269, a brefeldin A-cinnamate derivative, is an Arf1 inhibitor. CHNQD-01269 exhibits potent cytotoxic activity against HepG2 and BEL-7402 cells, with IC₅₀ values of 0.29 and 0.84 μM, respectively. CHNQD-01269 is indicated for hepatocellular carcinoma (HCC) research.

Myristoylated ARF6 (2-13) blocks MyD88–ARNO–ARF6–signaling axis by deactivating ARF6.

Bragsin1 (Standard) is the analytical standard of Bragsin1 (HY-111549). This product is intended for research and analytical applications. 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.