Chemical Structure : KDT-11
CAS No.:
KDT-11
(KDT11)
Catalog No.: PC-21187Not For Human Use, Lab Use Only.
KDT-11 is a specific, reversible peptidomimetic binder inhibitor of Rpn-13 with binding KD of 3 uM, selectively inhibit proliferation of a broad range of cancer cell lines (NCI60, IC50=5 uM), but not non-malignant cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
KDT-11 is a specific, reversible peptidomimetic binder inhibitor of Rpn-13 with binding KD of 3 uM, selectively inhibit proliferation of a broad range of cancer cell lines (NCI60, IC50=5 uM), but not non-malignant cells.
KDT-11 does not inhibit any of the known protein-protein interactions involving Rpn13, but blunts the ability of Rpn13 to activate the deubiquitylase activity of Uch37 in vitro.
KDT-11 blocks cell cycle progression at the G0/G1 to S boundary and drives subsequent apoptosis.
KDT-11 is a reversible binder to the Pru doman of Rpn-13.
Physicochemical Properties
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M.Wt
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1178.93
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Formula
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C66H89ClFN7O9
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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N-(14-amino-12-((1R,2R)-2-(benzyloxy)cyclopentyl)-3-(4-chlorophenethyl)-6-((R)-1-cyclohexylethyl)-9-(3,4-dimethoxyphenethyl)-2,5,8,11,14-pentaoxo-3,6,9,12-tetraazatetradecyl)-N-((R)-1-cyclohexylethyl)-2-((2-fluorobenzyl)(methyl)amino)acetamide
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References
1. Paige Dickson, et al. Cell Chem Biol. 2020 Nov 19;27(11):1383-1395.e5.
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