565725-M

SecinH3

A cell-permeable triazolo compound that acts as a Sec7 domain-binding, selective antagonist against cytohesin family small GEFs.

• Synonym(e): SecinH3, N-(4-(5-(1,3-Benzodioxol-5-yl)-3-methoxy-1H-1,2,4-triazol-1-yl)phenyl)-2-(phenylthio)acetamide, Cytohesin Inhibitor I
• Empirische Formel (Hill-System): C₂₄H₂₀N₄O₄S
• CAS-Nummer: 853625-60-2
• Molekulargewicht: 460.51
• UNSPSC-Code: 12352202
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 2-8°C
• InChI: 1S/C24H20N4O4S/c1-30-24-26-23(16-7-12-20-21(13-16)32-15-31-20)28(27-24)18-10-8-17(9-11-18)25-22(29)14-33-19-5-3-2-4-6-19/h2-13H,14-15H2,1H3,(H,25,29)
• InChIKey: QPGYAMIHXLCFTJ-UHFFFAOYSA-N

Beschreibung

Allgemeine Beschreibung

A cell-permeable triazolo compound that acts as a Sec7 domain-binding (K_d ≤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. Wirkung

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

Warnhinweis

Toxicity: Irritant (B)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

Hafner, M., et al. 2006. Nature444, 941.
Fuss, B., et al. 2006. Nature444, 945.

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable