A 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.
Biochem/physiol Actions
Kd ≤250 nM for Sec7 from human cytohesins 1-3; IC50 ≤5.6 µM in ARF1 GDP/GTP exchange assays using human cytohesin 3, as well as murine and Drosophila homologues
Primary Target Cytohesin
Warning
Toxicity: Irritant (B)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Hafner, M., et al. 2006. Nature444, 941. Fuss, B., et al. 2006. Nature444, 945.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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