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Legumain inhibitor 38u

Chemical Structure : Legumain inhibitor 38u

CAS No.: 1203212-36-5

Legumain inhibitor 38u (AEP inhibitor 38u)

Catalog No.: PC-20812Not For Human Use, Lab Use Only.

Legumain inhibitor 38u is a selective inhibitor of asparagine endopeptidase (AEP, Legumain) with IC50 of 160 nM, inhibits cancer metastasis.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Legumain inhibitor 38u is a selective inhibitor of asparagine endopeptidase (AEP, Legumain) with IC50 of 160 nM, inhibits cancer metastasis.
Legumain inhibitor 38u displays >1000-fold selectivity over other related major cysteine proteases (cathepsin-L, cathepsin-S, caspase-3 and caspase-8, all IC50s >150 uM).
Legumain inhibitor 38u blocks cancer cell invasion without impinging on the cell viability, Legumain inhibitor 38u (2 uM) significantly inhibits invasion of highly metastatic human breast cancer cell lines.
Legumain inhibitor 38u (3-10 mg/kg, oral gavage, 42 days) completely prevents breast-to-lung metastasis in vivo, does not exhibit toxic effects in mice.
Legumain inhibitor 38u inhibits AEP cleavage of MMP-2 in vitro and in vivo.

Physicochemical Properties

M.Wt 240.28
Formula C9H12N4O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(N1CC)N(C)C2=C(N(C)C(S)=N2)C1=O

References

1. Qi Qi, et al. J Med Chem. 2017 Sep 14;60(17):7244-7255.

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