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Capzimin

Chemical Structure : Capzimin

CAS No.: 2084867-65-0

Capzimin (Rpn11 inhibitor 3027)

Catalog No.: PC-60898Not For Human Use, Lab Use Only.

Capzimin (Rpn11 inhibitor 3027) is a derivative of 8TQ, and potent and specific inhibitor of proteasome isopeptidase Rpn11 (PSMD14) with IC50 of 0.34 uM, >7-fold improved potency over 8TQ (quinoline-8-thiol).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Capzimin (Rpn11 inhibitor 3027) is a derivative of 8TQ, and potent and specific inhibitor of proteasome isopeptidase Rpn11 (PSMD14) with IC50 of 0.34 uM, >7-fold improved potency over 8TQ (quinoline-8-thiol).
Capzimin shows >5-fold selectivity for Rpn11 over the related JAMM proteases and >2 logs less activity towards metalloenzymes (HDAC6, MMP2, MMP12, and carbonic anhydrase II).
Capzimin stabilizes proteasome substrates, induced an unfolded protein response, and blocks proliferation of cancer cells (HCT116 GI50=2.0 uM), including bortezomib-resistant retinal pigment epithelial cells.

Physicochemical Properties

M.Wt 315.409
Formula C15H13N3OS2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

8-Mercapto-N-(2-(thiazol-2-yl)ethyl)quinoline-3-carboxamide

References

1. Li J, et al. Nat Chem Biol. 2017 May;13(5):486-493.

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