Biological Activity
Rho GTPase inhibitor (Kd = 354 nM). Inhibits binding of RhoA to guanine nucleotide exchange factors (GEFs) including LARG, DBL, LBC, p115 RhoGEF and PDZ RhoGEF. Has no effect on the binding of Rac1 or Cdc42 to their respective GEFs. Suppresses RhoA/C-mediated breast cancer cell migration and invasion in vitro. Also induces neurite outgrowth in synergy with NGF.
Technical Data
| M. Wt | 394.86 |
| Formula | C20H18N6O.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1281870-42-5 |
| PubChem ID | 44662615 |
| InChI Key | SFRGBDFQSLZYLF-GRYLRVQNSA-N |
| Smiles | N[C@@H](C(N/N=C/C3=CC=C(N=CC=N4)C4=C3)=O)CC2=CNC1=CC=CC=C12.Cl |
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 | 39.49 | 100 | |
| water | 7.9 | 20mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 394.86. 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 | 2.53 mL | 12.66 mL | 25.33 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.07 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Shang et al (2013) Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc.Natl.Acad.Sci.U.S.A. 110 3155 PMID: 23382194
Shang et al (2012) Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem.Biol. 19 699 PMID: 22726684
Keywords: Rhosin hydrochloride, supplier, Rho, GTPases, inhibitors, inhibits, guanine, nucleotide, exchange, factors, GEF, GTPase, G, Proteins, (Small), GTPase, Tocris Bioscience
