Zetomipzomib (KZR-616) | LMP7/LMP2 inhibitor | Probechem Biochemicals

Chemical Structure : Zetomipzomib

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Zetomipzomib (KZR-616, KZR616)

货号: PC-38434Not For Human Use, Lab Use Only.

Zetomipzomib (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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生物&药学活性

Zetomipzomib (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	586.68
分子式	C30H42N4O8
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

参考文献

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

Zetomipzomib (KZR-616, KZR616)

生物&药学活性

物理化学性质&存储条件

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Zetomipzomib (KZR-616, KZR616)

生物&药学活性

物理化学性质&存储条件

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