KZR-616 maleate

Modify Date: 2025-09-08 19:36:00

KZR-616 maleate structure	Common Name	KZR-616 maleate
	CAS Number	2170983-62-5	Molecular Weight	702.75
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₃₄H₄₆N₄O₁₂	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of KZR-616 maleate

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

Name	KZR-616 maleate

Description	KZR-616 maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 maleate has the potential for the research of multiple autoimmune diseases[1][2].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome
In Vitro	KZR-616 maleate also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1]. KZR-616 maleate is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 (HY-13207) and PR-924 (HY-123587)[3].
In Vivo	KZR-616 maleate (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. Animal Model: 7-8 week old female BALB/c mice (CAIA model)[1] Dosage: I.v.; Dosing was repeated on days 6, 8, 11, and 13 until for 15 day Administration: 5 mg/kg Result: Showed efficacy in the anticollagen antibody induced arthritis (CAIA) model.
References	[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.

Molecular Formula	C₃₄H₄₆N₄O₁₂
Molecular Weight	702.75
InChIKey	HVKAUVYFVFFXLW-MTOCQVLVSA-N
SMILES	COc1ccc(C(O)C(NC(=O)C(C)NC(=O)CN2CCOCC2)C(=O)NC(CC2=CCCC2)C(=O)C2(C)CO2)cc1.O=C(O)C=CC(=O)O

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Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Zetomipzomib maleate
Price: Check
Purity: 99.0%
Delivery: 10 Day
Contact: Yang
Email: sales@echemcloud.com

DC Chemicals Limited
China
Product Name: KZR-616 maleate
Price: ￥Inquiry/1g
Purity: 98.9%
Delivery: 1 Day
Contact: Tony Cao
Email: sales@dcchemicals.com

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The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.