L 006235

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Cat.No. 3066 - L 006235 | C24H30N6O2S | CAS No. 294623-49-7
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)
Datasheet
Citations
Reviews

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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


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Citations for L 006235

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