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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Proteasome-KDT-11
KDT-11

Chemical Structure : KDT-11

CAS No.:

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KDT-11 (KDT11)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 1178.93
分子式 C66H89ClFN7O9
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

1. Paige Dickson, et al. Cell Chem Biol. 2020 Nov 19;27(11):1383-1395.e5.

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