A potent and selective cathepsin L inhibitor
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Cathepsin L Inhibitor

Item No. 23249

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-[[(1S)-1-formyl-2-(4-hydroxyphenyl)ethyl]amino]-2-oxo-1-(phenylmethyl)ethyl]-carbamic acid, phenylmethyl ester
CAS Number
167498-29-5
Synonyms
  • SB 412515
Molecular Formula
C26H26N2O5
Formula Weight
446.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/ml
λmax
209 nm
SMILES
OC1=CC=C(C[C@@H](C=O)NC([C@H](CC2=CC=CC=C2)NC(OCC3=CC=CC=C3)=O)=O)C=C1
InChi Code
InChI=1S/C26H26N2O5/c29-17-22(15-20-11-13-23(30)14-12-20)27-25(31)24(16-19-7-3-1-4-8-19)28-26(32)33-18-21-9-5-2-6-10-21/h1-14,17,22,24,30H,15-16,18H2,(H,27,31)(H,28,32)/t22-,24-/m0/s1
InChi Key
QVDJMLQSYRSZKC-UPVQGACJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Cathepsin L inhibitor is a potent inhibitor of cathepsin L (IC50 = 0.85 nM).1 It is selective for cathepsin L over calpain II and cathepsin B (IC50s = 184, and 85.1 nM, respectively). It is trypanocidal with an ED50 value of 45 nM against T. brucei that is well below the ED50 value of 21,500 nM for human HL-60 cells.2 Cathepsin L inhibitor completely suppresses osteoclastic pit formation on femur slices isolated from bovine cortical bone at a concentration of 1 μg/ml.1,3 In vivo, cathepsin L inhibitor (2.5-10 mg/kg) inhibits bone loss in a mouse model of osteoporosis in a dose-dependent manner.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Woo, J.-T., Sigeizumi, S., Yamaguchi, K., et al. Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L. Bioorganic Med. Chem. Lett. 5(14), 1501-1504 (1995).

    2. Nkemngu, N.J., Grande, R., Hansell, E., et al. Improved trypanocidal activities of cathepsin L inhibitors. Int. J. Antimicrob. Agents 22(2), 155-159 (2003).

    3. Woo, J.-T., Yamaguchi, K., Hayama, T., et al. Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo. Eur. J. Pharmacol. 300(1-2), 131-135 (1996).