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853625-60-2COc1nc(-c2ccc3c(c2)OCO3)n(-c2ccc(NC(=O)CSc3ccccc3)cc2)n1QPGYAMIHXLCFTJ-UHFFFAOYSA-N853625-60-2DTXSID80359866CHEMBL1731533CHEBI:92787안전 정보는 참고용이며, 공급업체의 물질안전보건자료(SDS), 관련 법규 및 전문가 평가를 대체하지 않습니다.
용도SecinH3 is a Sec7 cytohesin inhibitor.
일반 설명A cell-permeable triazolo compound that acts as a Sec7 domain-binding (Kd ≤250 nM for Sec7 from human cytohesins 1-3), selective antagonist against cytohesin family small GEFs (IC50 ≤5.6 μM in ARF1 GDP/GTP exchange assays using human cytohesin 3, as well as murine and Drosophila homologues). It inhibits large GEFs only at much higher concentrations (IC50 ≥65 μM in GDP/GTP exchange assays using hEFA6-S7 and yGea2-S7) and exhibits little activity against a panel of 10 commonly studied kinases or hSosII. Shown to effectively inhibit insulin signaling both in HepG2 cells in vitro and in Drosophila and mice in vivo.
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