Cat. No.: HY-101786

KZR-504

Name: KZR-504
Brand: MedChemExpress
SKU: HY-101786
Price: 450.00 USD
Availability: InStock
Rating: 5 (5 reviews)

5 Cited Publications

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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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté : 99.33%
CAS No.: 1629052-78-3
Formule: C₂₁H₂₃N₃O₆
Masse moléculaire:413.42

Stockage:

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

KZR-504 Chemical Structure

CAS No.: 1629052-78-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Publications (5)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC50: 51 nM (LMP2), 4.274 μM (LMP7)^[1].

Cellular Effect

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]

In Vivo

Evaluating the inhibition of LMP2, and antitargets LMP7 and β5, in mouse tissues reveals that KZR-504 (compound 12) is both selective and potent in vivo with >50% target inhibition achieved at >1 mg/kg in all tissues tested except brain^[1].

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
Masse moléculaire 413.42
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

-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)

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Journal Impact Factor

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

Solvant et solubilité

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4188 mL

12.0942 mL

24.1885 mL

5 mM

0.4838 mL

2.4188 mL

4.8377 mL

10 mM

0.2419 mL

1.2094 mL

2.4188 mL

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.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Johnson HWB, et al. Discovery of Highly Selective Inhibitors of the Immunoproteasome Low Molecular Mass Polypeptide 2 (LMP2) Subunit. ACS Med Chem Lett. 2017 Mar 9;8(4):413-417. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

KZR-504

5 Cited Publications

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KZR-504

Publications Citing Use of MedChemExpress (MCE) KZR-504