Biological Activity
Sec7-specific GEF inhibitor that displays selectivity for small GEFs of the cytohesin family (IC50 values are 2.4, 5.4, 5.4, 5.6, 5.6, 65 and > 100 μM for hCyh4, hCyh1, mCyh3, hCyh3, drosophila steppke, yGea2-S7 and hEFA6-S7 respectively). Inhibits insulin signaling via inhibition of insulin receptor substrate protein (IRS) phosphorylation.
Technical Data
| M. Wt | 460.5 |
| Formula | C24H20N4O4S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 853625-60-2 |
| PubChem ID | 1029232 |
| InChI Key | QPGYAMIHXLCFTJ-UHFFFAOYSA-N |
| Smiles | O=C(CSC5=CC=CC=C5)NC(C=C4)=CC=C4N1C(C2=CC(OCO3)=C3C=C2)=NC(OC)=N1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.05 | 100 | |
| ethanol | 4.61 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 460.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.17 mL | 10.86 mL | 21.72 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.34 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hafner et al (2006) Inhibition of cytohesins by secinH3 leads to hepatic insulin resistance. Nature 444 941 PMID: 17167487
Fuss et al (2006) The cytohesin Steppke is essential for insulin signalling in Drosophila. Nature 444 945 PMID: 17167488
Keywords: SecinH3, supplier, Sec7-specific, GEF, inhibitors, inhibits, cytohesins, hCyh4, hCyh1, mCyh3, hCyh3, drosophila, steppke, G, Proteins, Small, G, Proteins, (Small), GTPase, G, Proteins, (Small), Tocris Bioscience
