Rpn11 inhibitor 3021

Chemical Structure : Rpn11 inhibitor 3021

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货号: PC-60898Not For Human Use, Lab Use Only.

Rpn11 inhibitor 3021 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).

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

Rpn11 inhibitor 3021 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).
Rpn11 inhibitor 3021 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).
Rpn11 inhibitor 3021 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
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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.