KZR-504
Based on 5 publication(s) in Google Scholar
KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
For research use only. We do not sell to patients.
- Purity: 99.33%
- CAS No.: 1629052-78-3
- Formula: C21H23N3O6
- Molecular Weight:413.42
-
Storage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Covalent Screening Library
HY-L036
-
Ubiquitination Compound Library
HY-L050
-
Chemical Probe Library
HY-L063
-
Anti-Blood Cancer Compound Library
HY-L079
-
Heterocyclic Compound Library
HY-L138
-
Protease Inhibitor Library
HY-L147
-
Cysteine Targeted Covalent Library
HY-L153
-
Highly Selective Inhibitors Library
HY-L158
-
Anti-Hematopathy Compound Library
HY-L171
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
Publications Citing Use of MedChemExpress (MCE) KZR-504
More
Biological Activity
IC50: 51 nM (LMP2), 4.274 μM (LMP7)[1].
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| ARPE-19 | IC50 |
>30 μM
Compound: KZR-504
|
Cytotoxicity against human ARPE-19 cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
Cytotoxicity against human ARPE-19 cells assessed as reduction in cell viability incubated for 96 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay
|
[PMID: 38636481] |
| PBMC | IC50 |
>19.2 μM
Compound: 12; KZR-504
|
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-6 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
|
[PMID: 28435528] |
| PBMC | IC50 |
>25 μM
Compound: 12; KZR-504
|
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced GMCSF production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced GMCSF production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
|
[PMID: 28435528] |
| PBMC | IC50 |
>25 μM
Compound: 12; KZR-504
|
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced Il-1b production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced Il-1b production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
|
[PMID: 28435528] |
| PBMC | IC50 |
>25 μM
Compound: 12; KZR-504
|
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-8 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
|
[PMID: 28435528] |
| PBMC | IC50 |
>25 μM
Compound: 12; KZR-504
|
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNF-alpha production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced TNF-alpha production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
|
[PMID: 28435528] |
| PBMC | IC50 |
>25 μM
Compound: 12; KZR-504
|
Cytotoxicity against human PBMC assessed as decrease in cell viability by CellTiter-Glo assay
Cytotoxicity against human PBMC assessed as decrease in cell viability by CellTiter-Glo assay
|
[PMID: 28435528] |
| PBMC | IC50 |
>9.7 μM
Compound: 12; KZR-504
|
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-12/23 p40 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
Anti-inflammatory activity in human PBMC assessed as inhibition of LPS-induced IL-12/23 p40 production pretreated for 1 hr followed by LPS stimulation measured after 20 hrs
|
[PMID: 28435528] |
| RPMI-8226 | IC50 |
>10000 nM
Compound: KZR-504
|
Inhibition of LMP7/Beta 5 subunit chymotrypsin-like activity in human RPM18226 cell lysates using Suc-LLVY-AMC as substrate after 1 hr by fluorescence based microplate reader analysis
Inhibition of LMP7/Beta 5 subunit chymotrypsin-like activity in human RPM18226 cell lysates using Suc-LLVY-AMC as substrate after 1 hr by fluorescence based microplate reader analysis
|
[PMID: 32189500] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 1629052-78-3
-
Appearance Solid
-
Molecular Weight 413.42
-
Formula C21H23N3O6
-
Color White to off-white
-
SMILES
O=C(N[C@@H](CO)C(N[C@@H](CC1=CC=CC=C1)C([C@]2(CO2)C)=O)=O)C(N3)=CC=CC3=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Med Chem
α-Aminoboronic Acid Moieties in Boro Dipeptides Modulate Proteasome Subunit Selectivity and Provide Access to Compounds with Potent Anticancer and Anti-Inflammatory Activity. [Abstract]2025 Dec 25;68(24):26405-26417. PMID: 41344819 -
J Med Chem
Brain-Permeable Immunoproteasome-Targeting Macrocyclic Peptide Epoxyketones for Alzheimer's Disease. [Abstract]2024 May 9;67(9):7146-7157. PMID: 38636481 -
J Mol Biol
Immunoproteasome-specific Subunit Alterations as a Potential Therapeutic Target for Mitochondriopathies. [Abstract]2025 Sep 1;437(17):169229. PMID: 40414596 -
Oncol Res
Inhibition of Proteasome LMP2 Activity Suppresses Chil3 Expression in Mouse Colon Adenocarcinoma Tissue and Restrains Tumor Growth. [Abstract]2025 Aug 28;33(9):2573-2595. PMID: 40918453
Solvent & Solubility
DMSO : 100 mg/mL (241.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (279 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4188 mL | 12.0942 mL | 24.1885 mL | 60.4712 mL |
| 5 mM | 0.4838 mL | 2.4188 mL | 4.8377 mL | 12.0942 mL | |
| 10 mM | 0.2419 mL | 1.2094 mL | 2.4188 mL | 6.0471 mL | |
| 15 mM | 0.1613 mL | 0.8063 mL | 1.6126 mL | 4.0314 mL | |
| 20 mM | 0.1209 mL | 0.6047 mL | 1.2094 mL | 3.0236 mL | |
| 25 mM | 0.0968 mL | 0.4838 mL | 0.9675 mL | 2.4188 mL | |
| 30 mM | 0.0806 mL | 0.4031 mL | 0.8063 mL | 2.0157 mL | |
| 40 mM | 0.0605 mL | 0.3024 mL | 0.6047 mL | 1.5118 mL | |
| 50 mM | 0.0484 mL | 0.2419 mL | 0.4838 mL | 1.2094 mL | |
| 60 mM | 0.0403 mL | 0.2016 mL | 0.4031 mL | 1.0079 mL | |
| 80 mM | 0.0302 mL | 0.1512 mL | 0.3024 mL | 0.7559 mL | |
| 100 mM | 0.0242 mL | 0.1209 mL | 0.2419 mL | 0.6047 mL |
KZR-504 Related Classifications
HY-101786 Related Classifications
Powered by Bioz