Biological Activity
Transglutaminase 2 (TG2) inhibitor (IC50 = 0.25 μM). Binds at GTPase site; reversible.
Compound Libraries
LDN 27219 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 408.5 |
| Formula | C20H16N4O2S2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 312946-37-5 |
| PubChem ID | 1150683 |
| InChI Key | WLBUICQBNZXIDJ-UHFFFAOYSA-N |
| Smiles | O=C(NN)CSC(N1C2=CC=CC=C2)=NC3=C(C(C4=CC=CC=C4)=CS3)C1=O |
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 | 40.85 | 100 | |
| ethanol | 2.04 | 5mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 408.5. 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 | 2.45 mL | 12.24 mL | 24.48 mL |
| 5 mM | 0.49 mL | 2.45 mL | 4.9 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Case and Stein (2007) Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor. Biochemistry 46 1106 PMID: 17240993
Prime et al (2012) Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease. J.Med.Chem. 55 1021 PMID: 22224594
Duval et al (2005) Structure-activity relationship study of novel tissue transglutaminase inhibitors. Bioorg.Med.Chem.Lett. 15 1885 PMID: 15780627
Keywords: LDN 27219, supplier, LDN27219, transglutaminases, 2, TG2, TGase, tissue, tTG, inhibits, inhibitors, reversible, Other, Transferases, Other, Transferases, Tocris Bioscience
