L 006235A reversible and potent cathepsin K inhibitor that displays more than a 4000 fold selectivity over cathepsins B, L and S

L 006235 (CAS 294623-49-7)

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Synonym: N-[1-[[(Cyanomethyl)amino]carbonyl] cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazo lyl]benzamide
Application: A reversible and potent cathepsin K inhibitor that displays more than a 4000 fold selectivity over cathepsins B, L and S
CAS Number: 294623-49-7
Purity: ≥98%
Molecular Weight: 466.6
Molecular Formula: C24H30N6O2S
* Refer to Certificate of Analysis for lot specific data (including water content).
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L 006235 is a reversible and potent cathepsin K inhibitor that displays more than a 4000 fold selectivity over cathepsins B, L and S.


References

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. Falgueyret et al (2005) Lysosomotropism of basic cathepsin K inhibitors contri

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM).
Storage :
Store at 4° C
Melting Point :
326.42° C (Predicted)
Boiling Point :
743.67° C (Predicted)
Density :
1.32 g/cm3 (Predicted)
Refractive Index :
n20D 1.64 (Predicted)
IC50 :
Cathepsin K : IC50 = 0.25 nM; Osteoclasts: IC50 = 5 nM; Cathepsin B: IC50 = 17 nM (human); Cathepsin S: IC50 = 318 nM (Mus musculus); Cathepsin L: IC50 = 340 nM (human); A20 (Sarcoma B-lymphocytes): IC50 = 6.2 µM (Mus musculus)
Ki Data :
Cathepsin K: Ki= 0.2 nM (Oryctolagus cuniculus); Cathepsin B: Ki= 1 µM (human); Cathepsin L: Ki= 6 µM (human); Cathepsin S: Ki= 47 µM (human)
pK Values :
pKa: 12.07 (Predicted), pKb: 7.06 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9912381
MDL Number :
MFCD18086856
SMILES :
CN1CCN(CC1)C2=NC(=CS2)C3=CC=C(C=C3)C(=O)NC4(CCCCC4)C(=O)NCC#N

Download SDS (MSDS)

Certificate of Analysis

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