Bragsin1 |
Katalog-Nr.GC65306 |
Bragsin1 ist ein potenter, selektiver und nicht kompetitiver Inhibitor des ArfGEF. BRAG2 hemmt die Arf-GTPase-Aktivierung mit einem IC50 von 3 μM. Bragsin1 bindet an die PH-DomÄne von BRAG2 und ist ein nicht-kompetitiver GrenzflÄcheninhibitor. Bragsin1 hat keine Wirkung auf die Sec7-DomÄne menschlicher ArfGEFs. Anti-Krebs-AktivitÄt.
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Cas No.: 369631-68-5
Sample solution is provided at 25 µL, 10mM.
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[1].
[1]. Nawrotek A, et al. PH-domain-binding inhibitors of nucleotide exchange factor BRAG2 disrupt Arf GTPase signaling. Nat Chem Biol. 2019 Feb 11. doi: 10.1038/s41589-019-0228-3.
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