الصفحة الرئيسية>>Signaling Pathways>> Ubiquitination/ Proteasome>> Proteasome>>Rpn11-IN-1

Rpn11-IN-1 (Synonyms: Capzimin intermediate)

رقم الكتالوجGC32407

Rpn11-IN-1 (Capzimin وسيط) هو مثبط قوي وانتقائي للوحدة الفرعية البروتوزومية Rpn11 مع IC50 من 390 نانومتر

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Rpn11-IN-1 التركيب الكيميائي

Cas No.: 2084867-65-0

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Sample solution is provided at 25 µL, 10mM.

Description Protocol Chemical Properties Product Documents Related Products

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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