Bragsin1 |
| カタログ番号GC65306 |
Bragsin1 は ArfGEF BRAG2 の強力な選択的かつ非競合的な阻害剤であり、Arf GTPase の活性化を 3 μM の IC50 で阻害します。 Bragsin1 は BRAG2 の PH ドメインに結合し、非競合的な界面阻害剤です。 Bragsin1 は、ヒト ArfGEF の Sec7 ドメインには影響しません。抗がん作用。
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Cas No.: 369631-68-5
Sample solution is provided at 25 µL, 10mM.
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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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