2170983-62-5
2170983-62-5 structure
- Name: KZR-616 maleate
- Chemical Name: KZR-616 maleate
- CAS Number: 2170983-62-5
- Molecular Formula: C34H46N4O12
- Molecular Weight: 702.75
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Proteasome
- Create Date: 2021-09-10 09:40:09
- Modify Date: 2024-01-09 17:09:52
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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 |
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| 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]. |
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| Related Catalog | |
| 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 |
| Molecular Formula | C34H46N4O12 |
|---|---|
| Molecular Weight | 702.75 |