Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.

Product information

CAS Number: 2084867-65-0

Molecular Weight: 315.41

Formula: C15H13N3OS2

Chemical Name: 8-sulfanyl-N-[2-(1,3-thiazol-2-yl)ethyl]quinoline-3-carboxamide

Smiles: O=C(NCCC1=NC=CS1)C1=CN=C2C(S)=CC=CC2=C1

InChiKey: MYNGHZGMRXNEEH-UHFFFAOYSA-N

InChi: InChI=1S/C15H13N3OS2/c19-15(17-5-4-13-16-6-7-21-13)11-8-10-2-1-3-12(20)14(10)18-9-11/h1-3,6-9,20H,4-5H2,(H,17,19)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

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.

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