565725-M

SecinH3

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

• Sinonimo/i: 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
• Formula empirica (notazione di Hill): C₂₄H₂₀N₄O₄S
• Numero CAS: 853625-60-2
• Peso molecolare: 460.51
• Codice UNSPSC: 12352202
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 50 mg/mL
• Temperatura di conservazione: 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); QPGYAMIHXLCFTJ-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Attenzione

Toxicity: Irritant (B)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable