Zetomipzomib

Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases[1][2].

Product Specifications

CAS Number

[1629677-75-3]

Product Name Alternative

KZR-616

UNSPSC

12352005

Target

Proteasome

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/kzr-616.html

Purity

99.89

Solubility

DMSO : 50 mg/mL

Smiles

O=C(N[C@@H](CC1=CCCC1)C([C@]2(C)OC2)=O)[C@@H](NC([C@@H](NC(CN3CCOCC3)=O)C)=O)[C@H](O)C4=CC=C(OC)C=C4

Molecular Formula

C30H42N4O8

Molecular Weight

586.68

References & Citations

[1]Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R) - 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) propenamide) . J Med Chem. 2018 Dec 27;61 (24) :11127-11143.|[2]Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE) . Annals of the Rheumatic Diseases 2018;77:685.|[3]Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.