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Submit ReviewL 006235
Description: Potent cathepsin K inhibitor
Chemical Name: N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide
Purity: ≥98% (HPLC)
Biological Activity for L 006235
L 006235 is a potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. Displays reduced selectivity in cell-based assays possibly due to lysosomal accumulation. Reduces collagen breakdown and promotes bone deposition in vivo. Orally active and has intrinsic fluorescence.
Compound Libraries for L 006235
L 006235 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. Find out more about compound libraries available from Tocris.
Technical Data for L 006235
| M. Wt | 466.6 |
| Formula | C24H30N6O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 294623-49-7 |
| PubChem ID | 9912381 |
| InChI Key | FIVYCSWOCXEWSE-UHFFFAOYSA-N |
| Smiles | O=C(C2=CC=C(C3=CSC(N4CCN(C)CC4)=N3)C=C2)NC1(CCCCC1)C(NCC#N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for L 006235
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.66 | 100 |
Preparing Stock Solutions for L 006235
The following data is based on the product molecular weight 466.6. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 2.14 mL | 10.72 mL | 21.43 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.29 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.14 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets for L 006235
References for L 006235
References are publications that support the biological activity of the product.
Palmer et al (2005) Design and synthesis of tri-ring P3 benamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J.Med.Chem. 48 7520 PMID: 16302794
Falgueyret et al (2005) Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J.Med.Chem. 48 7535 PMID: 16302795
Desmarais et al (2008) Effects of cathepsin K inhibitors basicity on in vivo off-target activities. Mol.Pharmacol. 73 147 PMID: 17940194
If you know of a relevant reference for L 006235, please let us know.
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