WZ-1831
WZ-1831 is a selective inhibitor of the constitutive proteasome β5c subunit (IC50 0.01 μM). WZ-1831 exhibits anticancer activity against multiple myeloma. WZ-1831 synergizes with the β5i-selective inhibitor PKS21265 to induce cytotoxicity. WZ-1831 can be used for research on multiple myeloma.
For research use only. We do not sell to patients.
- CAS No.: 2892822-24-9
- Formula: C25H29BN4O6
- Molecular Weight:492.33
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MM1.S | EC50 |
0.14 μM
|
Cytotoxicity against human multiple myeloma MM.1S cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer/Glo assay.
Cytotoxicity against human multiple myeloma MM.1S cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer/Glo assay.
|
36608337 |
| RPMI-8226 | EC50 |
2.9 μM
|
Cytotoxicity against human multiple myeloma RPMI8226 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer/Glo assay.
Cytotoxicity against human multiple myeloma RPMI8226 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer/Glo assay.
|
36608337 |
| HepG2 | EC50 |
45 μM
|
Cytotoxicity against human liver hepatocellular carcinoma HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer/Glo assay.
Cytotoxicity against human liver hepatocellular carcinoma HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by Cell-titer/Glo assay.
|
36608337 |
| PBMC | EC50 |
>50 μM
|
Cytotoxicity against human peripheral blood mononuclear cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay.
Cytotoxicity against human peripheral blood mononuclear cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay.
|
36608337 |
In Vitro
WZ-1831 is a highly selective inhibitor of the constitutive proteasome β5c subunit with an IC50 of 10 nM, exhibiting 700-fold selectivity over the immunoproteasome β5i subunit[1].
WZ-1831 (11.1-100 μM) is specific for proteasome inhibition and does not inhibit cathepsin L, trypsin, or chymotrypsin at concentrations up to 100 μM[1].
WZ-1831 (72 h) is not cytotoxic to peripheral blood mononuclear cells (PBMCs), with an EC50 > 50 μM after 72 hours[1].
WZ-1831 (72 h) effectively kills multiple myeloma MM.1S cells (EC50 = 0.06 μM), but shows weaker activity against hepatocellular carcinoma HepG2 cells (EC50 = 3.2 μM), and has reduced potency against another multiple myeloma cell line RPMI8226 (EC50 = 2.3 μM)[1].
WZ-1831 (1.25 μM; 3-5 h) does not induce ROS in dermal fibroblasts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:MM.1S and RPMI8226 cells
-
Concentration:Various concentrations
-
Incubation Time:72 h
-
Result:In the presence of β5i-selective inhibitor PKS21265, the EC50 of WZ-1831 was shifted by 6-fold against MM.1S cells and by 10-fold against RPMI8226 cells.
Chemical Information
-
CAS No. 2892822-24-9
-
Molecular Weight 492.33
-
Formula C25H29BN4O6
-
SMILES
OB(O)C1=CC=CC(CNC([C@H](CC(NC(C)(C)C)=O)NC(C(C2=CNC3=CC=CC=C23)=O)=O)=O)=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
-
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
[1]. Zhan W, et al. Discovery of Highly Selective Inhibitors of the Human Constitutive Proteasome β5c Chymotryptic Subunit. Journal of medicinal chemistry. 2023 Jan 26;66(2):1172-1185. [Content Brief]
[2]. Laurent P, et al. The immunoproteasome regulates ILC2 responses by modulating mitochondrial capacity. Proceedings of the National Academy of Sciences of the United States of America. 2025 Nov 25;122(47):e2518190122. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)