GC7 Sulfate, the sulfate salt of GC-7 (N1-guanyl-1,7-diaminoheptane), is a novel and potent deoxyhypusine synthase (DHPS) inhibitor that inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins.
Physicochemical Properties
| Molecular Formula | C8H22N4O4S |
| Molecular Weight | 270.349680423737 |
| Exact Mass | 270.14 |
| Elemental Analysis | C, 35.54; H, 8.20; N, 20.72; O, 23.67; S, 11.86 |
| CAS # | 150417-90-6 |
| PubChem CID | 131842088 |
| Appearance | White to off-white solid powder |
| Hydrogen Bond Donor Count | 5 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 7 |
| Heavy Atom Count | 17 |
| Complexity | 200 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | S(O)(O)(=O)=O.C(CNC(N)=N)CCCCCN |
| InChi Key | MDDOWYFCKAAANU-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C8H20N4.H2O4S/c9-6-4-2-1-3-5-7-12-8(10)11;1-5(2,3)4/h1-7,9H2,(H4,10,11,12);(H2,1,2,3,4) |
| Chemical Name | 2-(7-aminoheptyl)guanidine;sulfuric acid |
| Synonyms | N1-Guanyl-1,7-diaminoheptane; GC7 (sulfate) |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | DHPS; p21 |
| ln Vitro | GC7 Sulfate is a deoxyhypusine synthase (DHPS) inhibitor that exhibits the ability to suppress MYCN-amplified and chemotherapy-resistant NB cell proliferation. It also modulates multiple cell cycle-regulating proteins and initiates arrest through the p21/Cdk4/Rb signaling axis, even when MYCN is present.[1] |
| Cell Assay | The MTS assay kit is used to assess cell viability in compliance with the manufacturer's instructions. To summarize, cells are treated with GC7 Sulfate in 96-well plates for 72 hours at different concentrations (0.1 to 100 μM). Following this, they are immediately incubated with the MTS dye reagent for 1 hour at 37°C in 5% CO2 atmosphere. Using a reader, the absorbance is measured at 490 nm. |
| References |
[1]. Deoxyhypusine synthase (DHPS) inhibitor GC7 induces p21/Rb-mediated inhibition of tumor cell growth and DHPS expression correlates with poor prognosis in neuroblastoma patients. Cell Oncol (Dordr). 2014 Dec;37(6):387-98. [2]. N1-guanyl-1,7-diaminoheptane (GC7) enhances the therapeutic efficacy of doxorubicin by inhibiting activation of eukaryotic translation initiation factor 5A2 (eIF5A2) and preventing the epithelial-mesenchymal transition in hepatocellular carcinoma cells. Exp Cell Res. 2013 Oct 15;319(17):2708-17. |
Solubility Data
| Solubility (In Vitro) | Water : 3 mg/mL |
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (18.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C). (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6989 mL | 18.4945 mL | 36.9891 mL | |
| 5 mM | 0.7398 mL | 3.6989 mL | 7.3978 mL | |
| 10 mM | 0.3699 mL | 1.8495 mL | 3.6989 mL |