Rpn11-IN-1 (Synonyms: Capzimin intermediate) |
| Catalog No.GC32407 |
Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
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Cas No.: 2084867-65-0
Sample solution is provided at 25 µL, 10mM.
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Rpn11-IN-1 is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
Rpn11 is a Zn2+-dependent metalloisopeptidase that hydrolyzes ubiquitin from tagged proteins that are trafficked to the proteasome for degradation. When inhibition of Rpn11-IN-1 (Compound 35) against Rpn11 is measured in the presence of Zn(cyclen)2+ (100 μM), a significant loss in activity against Rpn11 is observed (IC50=77.4 μM vs. 0.39 μM). The observed IC50 value shift is attributed to the ability of Zn(cyclen)2+ to compete/titrate Rpn11-IN-1 away from Rpn11. Rpn11-IN-1 blocks proliferation of tumor cells in culture. Rpn11-IN-1 has an IC50 of 2.1 μM and 3.8 μM against 293T and A549 cells, respectively[1].
[1]. Perez C, et al. Discovery of an Inhibitor of the Proteasome Subunit Rpn11. J Med Chem. 2017 Feb 23;60(4):1343-1361.
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