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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Proteasome-Zetomipzomib maleate
Zetomipzomib maleate

Chemical Structure : Zetomipzomib maleate

CAS No.: 2170983-62-5

Zetomipzomib maleate (KZR-616 maleate)

货号: PC-28687Not For Human Use, Lab Use Only.

Zetomipzomib maleate (KZR-616) is a first-in-class inhibitor of immunoproteasome, dually inhibits immunoproteasome subunits LMP7 (IC50, 39/57 nM, hLMP7/mLMP7) and LMP2 (IC50, 131/179 nM, hLMP2/mLMP2).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Zetomipzomib maleate (KZR-616) is a first-in-class inhibitor of immunoproteasome, dually inhibits immunoproteasome subunits LMP7 (IC50, 39/57 nM, hLMP7/mLMP7) and LMP2 (IC50, 131/179 nM, hLMP2/mLMP2).
Zetomipzomib (KZR-616) also potently inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM), and maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells.
Zetomipzomib (KZR-616) exhibits potent cytokine expression inhibition and in vivo efficacy in an inflammatory disease model.

物理化学性质&存储条件

分子量 702.76
分子式 C34H46N4O12
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

(2S,3R)-N-((S)-3-(Cyclopent-1-en-1-yl)-1-((R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanamide maleate

参考文献

1. Johnson HWB, et al. J Med Chem. 2018 Dec 27;61(24):11127-11143.

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