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BJP-06-005-3

Chemical Structure : BJP-06-005-3

CAS No.: 2400958-08-7

BJP-06-005-3

Catalog No.: PC-72215Not For Human Use, Lab Use Only.

BJP-06-005-3 is a potent, selective, covalent, cell-permeable peptide Pin1 inhibitor (Ki=15 nM) that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BJP-06-005-3 is a potent, selective, covalent, cell-permeable peptide Pin1 inhibitor (Ki=15 nM) that covalently target Cys113, a highly conserved cysteine located in the Pin1 active site.
BJP-06–005-3 potently inhibited Pin1 catalytic activity with an apparent Ki of 48 nM in PPIase assays.
BJP-06-005-3 reduced cell viability cross a panel of cancer cell lines in a dose- and time-dependent manner.
BJP-06-005-3 increased phospho-CDK1 Tyr15 in Pin1-WT PDAC cell, but not in Pin1 KO cells, affected expression of downstream Pin1 substrates, increased c-Myc protein levels, cooperated with KRASG12V degradation.

Physicochemical Properties

M.Wt 738.283
Formula C37H48ClN7O7
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

ethyl (S)-2-((S)-2-((S)-1-(N-(2-chloroacetyl)-N-methyl-L-phenylalanyl)piperidine-2-carboxamido)-3-(1H-indol-3-yl)propanamido)-5-ureidopentanoate

References

1. Benika J Pinch, et al. Nat Chem Biol. 2020 Sep;16(9):979-987.

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