Rpn11 inhibitor 3027 | Rpn11 inhibitor | Probechem Biochemicals

Chemical Structure : Rpn11 inhibitor 3027

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Rpn11 inhibitor 3027 (Capzimin)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	315.409
分子式	C15H13N3OS2
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	8-Mercapto-N-(2-(thiazol-2-yl)ethyl)quinoline-3-carboxamide

参考文献

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

Rpn11 inhibitor 3027 (Capzimin)

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物理化学性质&存储条件

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Rpn11 inhibitor 3027 (Capzimin)

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