Bortezomib
Based on 261 publication(s) in Google Scholar
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
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- Reinheit: 99.80%
- CAS. Nr.: 179324-69-7
- Formel: C19H25BN4O4
- Molecular Weight:384.24
-
Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Bortezomib
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- Int Immunopharmacol. 2020 Mar 3;82:106259. [Abstract]
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- Mol Pharm. 2025 Aug 4;22(8):4865-4878. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- Front Cell Dev Biol. 2021 Mar 30:9:633259. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2023 Oct;1869(7):166767. [Abstract]
- FASEB J. 2021 Aug;35(8):e21800. [Abstract]
- J Cell Mol Med. 2021 Mar;25(6):3124-3135. [Abstract]
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- iScience. 2022 Aug 4;25(9):104844. [Abstract]
- iScience. 2022 Jul 19;25(8):104781. [Abstract]
- J Inflamm Res. 2022 Feb 15;15:1027-1046. [Abstract]
- Transl Oncol. 2022 Apr;18:101362. [Abstract]
- J Cell Physiol. 2025 Jan;240(1):e31459. [Abstract]
- Virol Sin. 2019 Oct;34(5):572-582. [Abstract]
- J Biol Chem. 2026 Jan 20:111182. [Abstract]
- Sci Rep. 2025 May 9;15(1):16209. [Abstract]
- Sci Rep. 2022 Nov 5;12(1):18811. [Abstract]
- Aging. 2020 Nov 25;12(24):25730-25743. [Abstract]
- J Virol. 2025 Nov 25:e0164825. [Abstract]
- Chem Res Toxicol. 2024 Jun 17;37(6):1062-1069. [Abstract]
- J Virol. 2022 Feb 9;96(3):e0110321. [Abstract]
- Cell Signal. 2025 Dec 19:139:112333. [Abstract]
- J Photochem Photobiol B. 2025 Apr 3:267:113162. [Abstract]
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- Cell Signal. 2024 Nov 29:127:111533. [Abstract]
- Mol Cell Biochem. 2024 Apr;479(4):843-857. [Abstract]
- Proteomes. 2025 Nov 25;13(4):63. [Abstract]
- Heliyon. 2023 Feb 1;9(2):e13397. [Abstract]
- Epigenomes. 2026 Feb 23;10(1):14. [Abstract]
- Exp Cell Res. 2024 Jun 5:114117. [Abstract]
- Exp Cell Res. 2023 Sep 15;430(2):113718. [Abstract]
- Med Oncol. 2020 Nov 19;37(12):116. [Abstract]
- Exp Cell Res. 2020 Aug 1;393(1):112054. [Abstract]
- ChemMedChem. 2026 Jun 26;21(12):e70328. [Abstract]
- J Immunol. 2023 Mar 15;210(6):786-794. [Abstract]
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- PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]
- BMC Cancer. 2018 Oct 11;18(1):971. [Abstract]
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- Am J Cancer Res. 2020 Nov 1;10(11):3752-3764. [Abstract]
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Biologische Aktivität
|
20S proteasome subunit β5 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 5TGM1 | IC50 |
6.78 nM
Compound: PS-341, Bortezomib
|
Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay
Cytotoxicity against mouse 5TGM1 cells after 48 to 72 hrs by SRB assay
|
[PMID: 24119559] |
| 786-0 | GI50 |
1.44 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human 786-0 cells
Growth inhibition of human 786-0 cells
|
[PMID: 24946214] |
| A2780 | IC50 |
1.7 nM
Compound: 1, bortezomib
|
Cytotoxicity against human A2780 cells
Cytotoxicity against human A2780 cells
|
[PMID: 18247547] |
| A2780 | IC50 |
28.9 nM
Compound: Bortezomib
|
Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay
Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay
|
[PMID: 28182990] |
| A-431 | IC50 |
28.2 nM
Compound: Bortezomib
|
Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| A498 | GI50 |
0.48 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human A498 cells
Growth inhibition of human A498 cells
|
[PMID: 24946214] |
| A549 | IC50 |
255 nM
Compound: bortezomib
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| A549 | IC50 |
6.7 nM
Compound: bortezomib
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| A549 | IC50 |
13.9 nM
Compound: bortezomib
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| A549 | GI50 |
3.09 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human A549/ATCC cells
Growth inhibition of human A549/ATCC cells
|
[PMID: 24946214] |
| A549 | IC50 |
2135.73 nM
Compound: PS-341
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| A549 | IC50 |
2.5 nM
Compound: Bortezomib
|
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 28182990] |
| A549 | IC50 |
92 nM
Compound: BTZ
|
Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay
Antiproliferative activity against human A549 cells after 72 hrs by Cell Titer-Glo assay
|
[PMID: 28191850] |
| A549 | IC50 |
2.14 μM
Compound: Bortezomib
|
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 28634039] |
| A549 | IC50 |
9.318 μM
Compound: Bortezomib
|
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
|
[PMID: 29426629] |
| A549 | IC50 |
0.62 μM
Compound: Bortezomib
|
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
|
[PMID: 38381886] |
| ACHN | GI50 |
0.79 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human ACHN cells
Growth inhibition of human ACHN cells
|
[PMID: 24946214] |
| ARH-77 | IC50 |
6.07 nM
Compound: Bortezomib
|
Cytotoxicity against human ARH77 cells after 72 hrs by MTS assay
Cytotoxicity against human ARH77 cells after 72 hrs by MTS assay
|
[PMID: 26965867] |
| ARH-77 | IC50 |
9.57 nM
Compound: Bortezomib
|
Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 29934218] |
| BEL-7404 tumor cell line | IC50 |
25.04 nM
Compound: PS-341
|
Antiproliferative activity against human Bel7404 cells after 72 hrs by MTT assay
Antiproliferative activity against human Bel7404 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| BGC-823 | IC50 |
880 nM
Compound: bortezomib
|
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| BGC-823 | IC50 |
2890 nM
Compound: Bortezomib
|
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
|
[PMID: 19747832] |
| BT-549 | GI50 |
0.55 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human BT549 cells
Growth inhibition of human BT549 cells
|
[PMID: 24946214] |
| BXPC-3 | IC50 |
11.8 nM
Compound: Bortezomib
|
Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay
Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay
|
[PMID: 19747832] |
| BXPC-3 | IC50 |
16.2 nM
Compound: bortezomib
|
Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay
Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| BXPC-3 | IC50 |
19.4 nM
Compound: bortezomib
|
Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay
Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| CAKI-1 | GI50 |
0.66 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human CAKI-1 cells
Growth inhibition of human CAKI-1 cells
|
[PMID: 24946214] |
| CAL-27 | IC50 |
4.73 μM
Compound: BTZ
|
Antiproliferative activity against human CAL-27 cells overexpressing HDAC4 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human CAL-27 cells overexpressing HDAC4 assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 37979441] |
| CAL-27 | IC50 |
7.6 μM
Compound: BTZ
|
Antiproliferative activity against human CAL-27 cells without HDAC4 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human CAL-27 cells without HDAC4 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 37979441] |
| Calu-6 | IC50 |
3.9 nM
Compound: Bortezomib
|
Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay
Inhibition of 26S proteasome beta5 subunit in human Calu6 cells using Suc-LLVY-aminoluciferin as substrate after 1hr by luminescence assay
|
10.1039/C2MD20060K |
| CCRF-CEM | GI50 |
0.35 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human CCRF-CEM cells
Growth inhibition of human CCRF-CEM cells
|
[PMID: 24946214] |
| CCRF-CEM | IC50 |
11 nM
Compound: Bortezomib
|
Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| CCRF-CEM | GI50 |
0.001 μM
Compound: Bortezomib
|
Antiproliferative activity against human CEM cells after 72 hrs by calcein AM staining based fluorescence assay
Antiproliferative activity against human CEM cells after 72 hrs by calcein AM staining based fluorescence assay
|
[PMID: 28441582] |
| COLO 205 | GI50 |
1.23 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human COLO205 cells
Growth inhibition of human COLO205 cells
|
[PMID: 24946214] |
| DLD-1 | IC50 |
0.0002 μM
Compound: Bortezomib, Velcade, PS-341
|
Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
|
[PMID: 22206869] |
| DLD-1 | IC50 |
0.0009 μM
Compound: Bortezomib, Velcade, PS-341
|
Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
|
[PMID: 22206869] |
| DLD-1 | IC50 |
0.2 nM
Compound: Bortezomib, Velcade, PS-341
|
Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
Inhibition of chymotrypsin-like activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Succinyl-Leu-Leu-Val-Tyr-AMC as substrate after 6 hrs by spectrofluorometric analysis
|
[PMID: 22206869] |
| DLD-1 | IC50 |
0.9 nM
Compound: Bortezomib, Velcade, PS-341
|
Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
Inhibition of peptide-glutamyl-peptide-hydrolyzing activity of 20S proteasome in human DLD1 cells transfected with 4Ub-Luc gene using Z-Leu-Leu-Glu-AMC as substrate after 6 hrs by spectrofluorometric analysis
|
[PMID: 22206869] |
| DU-145 | GI50 |
1.7 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human DU145 cells
Growth inhibition of human DU145 cells
|
[PMID: 24946214] |
| EA.hy 926 | IC50 |
0.09 μM
Compound: Bortezomib
|
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human EA.hy 926 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
|
[PMID: 38381886] |
| EKVX | GI50 |
3.02 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human EKVX cells
Growth inhibition of human EKVX cells
|
[PMID: 24946214] |
| GES1 | IC50 |
12.6 nM
Compound: PS-341
|
Antiproliferative activity against human GES-1 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human GES-1 cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| HCC 2998 | GI50 |
0.6 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HCC2998 cells
Growth inhibition of human HCC2998 cells
|
[PMID: 24946214] |
| HCT-116 | IC50 |
0.01 μM
Compound: bortezomib
|
Cytotoxicity against human HCT116 cells after 72 hrs by CCK-8 assay
Cytotoxicity against human HCT116 cells after 72 hrs by CCK-8 assay
|
[PMID: 23547757] |
| HCT-116 | IC50 |
5 nM
Compound: bortezomib
|
Inhibition of human HCT116 cell growth
Inhibition of human HCT116 cell growth
|
[PMID: 24524217] |
| HCT-116 | GI50 |
0.6 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HCT116 cells
Growth inhibition of human HCT116 cells
|
[PMID: 24946214] |
| HCT-116 | IC50 |
27 nM
Compound: Bortezomib
|
Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| HCT-116 | IC50 |
1.4 nM
Compound: PS-341
|
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| HCT-116 | IC50 |
0.001 μM
Compound: Bortezomib
|
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
|
[PMID: 28634039] |
| HCT-15 | GI50 |
1.51 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HCT15 cells
Growth inhibition of human HCT15 cells
|
[PMID: 24946214] |
| HEK293 | IC50 |
10 nM
Compound: 1, bortezomib
|
Inhibition of TNF-alpha-induced NF-kappaB activation in human HEK293 cells after 3 hrs by luciferase reporter gene assay
Inhibition of TNF-alpha-induced NF-kappaB activation in human HEK293 cells after 3 hrs by luciferase reporter gene assay
|
[PMID: 20875739] |
| HEK293 | IC50 |
0.014 μM
Compound: PS-341
|
Inhibition of NF-kappaB activity in TNF-alpha-induced human HEK293 cells after 30 mins by luciferase assay
Inhibition of NF-kappaB activity in TNF-alpha-induced human HEK293 cells after 30 mins by luciferase assay
|
[PMID: 21044847] |
| HEK293 | CC50 |
347 nM
Compound: 1a, Bortezomib
|
Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay
Cytotoxicity against human HEK293 cells after 24 hrs by MTT assay
|
[PMID: 21634429] |
| HEK293 | IC50 |
27 nM
Compound: 1a, Bortezomib
|
Inhibition of intracellular chymotrypsin-like activity of 20S proteasome in human HEK293 cells after 24 hrs by fluorescence plate reader
Inhibition of intracellular chymotrypsin-like activity of 20S proteasome in human HEK293 cells after 24 hrs by fluorescence plate reader
|
[PMID: 21634429] |
| HEK293 | IC50 |
14 μM
Compound: Bortezomib
|
Cytotoxicity against human HEK293 cells assessed as cell growth inhibition
Cytotoxicity against human HEK293 cells assessed as cell growth inhibition
|
[PMID: 33333398] |
| HEK293 | IC50 |
9.7 nM
Compound: Bortezomib
|
Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control
Inhibition of NFkappaB in HEK293 cells incubated for 1 hr prior to TNF-alpha challenge measured after 3 hrs by luciferase reporter gene assay relative to control
|
10.1039/C2MD20060K |
| HEK-293T | IC50 |
12 nM
Compound: BTZ
|
Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay
Antiproliferative activity against human 293T cells after 72 hrs by Cell Titer-Glo assay
|
[PMID: 28191850] |
| HeLa | IC50 |
0.02 μM
Compound: PS-341
|
Growth inhibition of human HeLa cells after 72 hrs by MTT assay
Growth inhibition of human HeLa cells after 72 hrs by MTT assay
|
[PMID: 19428245] |
| HeLa | IC50 |
92 nM
Compound: bortezomib
|
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| HeLa | GI50 |
168.1 μM
Compound: BTZ; Product S4
|
Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity in human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 32031798] |
| HeLa | IC50 |
>200 nM
Compound: Btz
|
Cytotoxicity against oleic acid-induced human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against oleic acid-induced human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 35059132] |
| HeLa | IC50 |
20 nM
Compound: Btz
|
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 35059132] |
| HepG2 | IC50 |
37.5 nM
Compound: bortezomib
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| HepG2 | IC50 |
7.5 nM
Compound: bortezomib
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| HepG2 | IC50 |
25.2 nM
Compound: bortezomib
|
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| HepG2 | IC50 |
1.61 nM
Compound: PS-341
|
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| HepG2 | EC50 |
0.01 μM
Compound: Bortezomib
|
Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells after 48 hrs by CellTiter-Glo assay
|
[PMID: 29800827] |
| HepG2 | GI50 |
100.6 μM
Compound: BTZ; Product S4
|
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 32031798] |
| HepG2 | EC50 |
0.013 μM
Compound: BTZ
|
Cytotoxicity against human HepG2 cells after 72 hrs by celltitre-glo assay
Cytotoxicity against human HepG2 cells after 72 hrs by celltitre-glo assay
|
[PMID: 36608337] |
| HET-1A | IC50 |
25.6 nM
Compound: PS-341
|
Antiproliferative activity against human HET-1A cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HET-1A cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| HL-60 | ED50 |
2.5 nM
Compound: bortezomib
|
Inhibition of chymotrypsin-like activity of proteasome in human HL60 cells assessed as free AMC level after 10 mins
Inhibition of chymotrypsin-like activity of proteasome in human HL60 cells assessed as free AMC level after 10 mins
|
[PMID: 19422206] |
| HL-60 | IC50 |
5.5 nM
Compound: bortezomib
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| HL-60 | IC50 |
6.9 nM
Compound: Bortezomib
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 19747832] |
| HL-60 | IC50 |
7.1 nM
Compound: bortezomib
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| HL-60 | IC50 |
3.5 nM
Compound: bortezomib
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| HL-60 | ED50 |
0.0025 μM
Compound: Bortezomib
|
Inhibition of chymotrypsin-like activity of purified human 20S proteasome in HL60 cells using N-succinyl-Leu-Leu-Val-Tyr-AMC as substrate pre-incubated for 10 mins by fluorimetric assay
Inhibition of chymotrypsin-like activity of purified human 20S proteasome in HL60 cells using N-succinyl-Leu-Leu-Val-Tyr-AMC as substrate pre-incubated for 10 mins by fluorimetric assay
|
[PMID: 21973101] |
| HL-60 | IC50 |
7.6 nM
Compound: PS-341
|
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| HL-60 | IC50 |
3.2 nM
Compound: Bortezomib
|
Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay
Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay
|
[PMID: 28182990] |
| HL-60 | IC50 |
0.008 μM
Compound: Bortezomib
|
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 28634039] |
| HL-60(TB) | GI50 |
1.9 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HL-60(TB) cells
Growth inhibition of human HL-60(TB) cells
|
[PMID: 24946214] |
| HOP-62 | GI50 |
4.47 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HOP62 cells
Growth inhibition of human HOP62 cells
|
[PMID: 24946214] |
| HOP-92 | GI50 |
1 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HOP92 cells
Growth inhibition of human HOP92 cells
|
[PMID: 24946214] |
| Hs-578T | GI50 |
1.02 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human Hs 578T cells
Growth inhibition of human Hs 578T cells
|
[PMID: 24946214] |
| HT-29 | ED50 |
>20 μM
Compound: Bortezomib
|
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
Cytotoxicity against human HT-29 cells after 3 days by sulforhodamine B assay
|
[PMID: 21973101] |
| HT-29 | GI50 |
0.95 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human HT-29 cells
Growth inhibition of human HT-29 cells
|
[PMID: 24946214] |
| HT-29 | IC50 |
3.2 nM
Compound: Btz
|
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 35059132] |
| HUVEC | IC50 |
11.2 nM
Compound: PS-341
|
Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay
Antiproliferative activity against HUVEC cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| IGROV-1 | GI50 |
2.24 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human IGROV1 cells
Growth inhibition of human IGROV1 cells
|
[PMID: 24946214] |
| K562 | GI50 |
1.17 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human K562 cells
Growth inhibition of human K562 cells
|
[PMID: 24946214] |
| K562 | GI50 |
0.007 μM
Compound: Bortezomib
|
Antiproliferative activity against human K562 cells after 72 hrs by calcein AM staining based fluorescence assay
Antiproliferative activity against human K562 cells after 72 hrs by calcein AM staining based fluorescence assay
|
[PMID: 28441582] |
| KB | IC50 |
59.5 nM
Compound: bortezomib
|
Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| KM12 | GI50 |
1.7 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human KM12 cells
Growth inhibition of human KM12 cells
|
[PMID: 24946214] |
| KM3/BTZ | IC50 |
226 nM
Compound: PS-341
|
Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay
Antiproliferative activity against bortezomib resistant human KM3/BTZ cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| L02 | IC50 |
55.5 nM
Compound: PS-341
|
Antiproliferative activity against human HL7702 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HL7702 cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| LOX IMVI | GI50 |
0.78 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human LOXIMVI cells
Growth inhibition of human LOXIMVI cells
|
[PMID: 24946214] |
| M14 | GI50 |
0.93 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human M14 cells
Growth inhibition of human M14 cells
|
[PMID: 24946214] |
| Malme-3M | GI50 |
0.45 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human MALME-3M cells
Growth inhibition of human MALME-3M cells
|
[PMID: 24946214] |
| MCF7 | GI50 |
0.55 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human MCF7 cells
Growth inhibition of human MCF7 cells
|
[PMID: 24946214] |
| MCF7 | IC50 |
0.025 μM
Compound: Bz
|
Antiproliferative activity against human MCF7 cells after 3 days by SRB assay
Antiproliferative activity against human MCF7 cells after 3 days by SRB assay
|
[PMID: 28557430] |
| MCF7 | IC50 |
18.37 μM
Compound: Bortezomib
|
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells after 72 hrs by SRB assay
|
[PMID: 29426629] |
| MDA-MB-231 | GI50 |
1.26 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human MDA-MB-231 cells
Growth inhibition of human MDA-MB-231 cells
|
[PMID: 24946214] |
| MDA-MB-231 | IC50 |
16.65 nM
Compound: PS-341
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| MDA-MB-231 | IC50 |
6.5 nM
Compound: Bortezomib
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
|
[PMID: 28182990] |
| MDA-MB-231 | IC50 |
0.017 μM
Compound: Bortezomib
|
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 28634039] |
| MDA-MB-231 | IC50 |
3.125 μM
Compound: Bortezomib
|
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
|
[PMID: 29426629] |
| MDA-MB-231 | IC50 |
0.003 μM
Compound: Bortezomib
|
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 24 hrs
|
[PMID: 33139111] |
| MDA-MB-231 | IC50 |
0.46 μM
Compound: Bortezomib
|
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
|
[PMID: 38381886] |
| MDA-MB-435 | GI50 |
0.44 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human MDA-MB-435 cells
Growth inhibition of human MDA-MB-435 cells
|
[PMID: 24946214] |
| MDA-MB-468 | GI50 |
1.48 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human MDA-MB-468 cells
Growth inhibition of human MDA-MB-468 cells
|
[PMID: 24946214] |
| MGC-803 | IC50 |
5.782 nM
Compound: PS-341
|
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| MGC-803 | IC50 |
0.008 μM
Compound: Bortezomib
|
Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay
Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay
|
[PMID: 28634039] |
| MKN-45 | IC50 |
7.15 nM
Compound: PS-341
|
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay
Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| MM1.S | IC50 |
2.5 nM
Compound: BTZ
|
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay
Antiproliferative activity against human MM1.S cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay
|
[PMID: 34445874] |
| MM1.S | IC50 |
0.0026 μM
Compound: Bortezomib
|
Antiproliferative activity against dexamethasone-sensitive human MM.1S cells assessed as reduction in cell viability measured after 72 hrs by XTT assay
Antiproliferative activity against dexamethasone-sensitive human MM.1S cells assessed as reduction in cell viability measured after 72 hrs by XTT assay
|
[PMID: 34969245] |
| MM1.S | IC50 |
0.0032 μM
Compound: Bortezomib
|
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 36512676] |
| MM1.S | EC50 |
0.002 μM
Compound: BTZ
|
Cytotoxicity against human MM1.S cells after 72 hrs by celltitre-glo assay
Cytotoxicity against human MM1.S cells after 72 hrs by celltitre-glo assay
|
[PMID: 36608337] |
| MOLT-4 | EC50 |
21 nM
Compound: 1, bortezomib
|
Inhibition of chymotrypsin-like activity of human 20S proteasome in Molt4 cells
Inhibition of chymotrypsin-like activity of human 20S proteasome in Molt4 cells
|
[PMID: 18247547] |
| MOLT-4 | EC50 |
21 nM
Compound: 8
|
Inhibition of chymotrypsin-like activity of 26S proteasome in human Molt4 cells using MeOSuc-Phe-Leu-Phe-AFC substrate
Inhibition of chymotrypsin-like activity of 26S proteasome in human Molt4 cells using MeOSuc-Phe-Leu-Phe-AFC substrate
|
[PMID: 22503349] |
| MOLT-4 | GI50 |
0.51 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human MOLT4 cells
Growth inhibition of human MOLT4 cells
|
[PMID: 24946214] |
| Multiple myeloma cancer stem cell | IC50 |
8.4 nM
Compound: BTZ
|
Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay
Antiproliferative activity against human multiple myeloma cancer stem cells after 72 hrs by MTT assay
|
[PMID: 30108696] |
| NCI/ADR-RES | GI50 |
12.3 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human NCI-ADR-RES cells
Growth inhibition of human NCI-ADR-RES cells
|
[PMID: 24946214] |
| NCI-H226 | GI50 |
0.46 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human NCI-H226 cells
Growth inhibition of human NCI-H226 cells
|
[PMID: 24946214] |
| NCI-H23 | GI50 |
1 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human NCI-H23 cells
Growth inhibition of human NCI-H23 cells
|
[PMID: 24946214] |
| NCI-H23 | IC50 |
0.01 μM
Compound: Btz
|
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
|
[PMID: 30964987] |
| NCI-H322M | GI50 |
17.8 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human NCI-H322M cells
Growth inhibition of human NCI-H322M cells
|
[PMID: 24946214] |
| NCI-H460 | IC50 |
115 nM
Compound: bortezomib
|
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| NCI-H460 | IC50 |
780 nM
Compound: bortezomib
|
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
Cytotoxicity against human H460 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| NCI-H460 | GI50 |
4.47 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human NCI-H460 cells
Growth inhibition of human NCI-H460 cells
|
[PMID: 24946214] |
| NCI-H522 | GI50 |
1.44 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human NCI-H522 cells
Growth inhibition of human NCI-H522 cells
|
[PMID: 24946214] |
| NCI-H727 | IC50 |
0.025 μM
Compound: Btz
|
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
|
[PMID: 30964987] |
| NCI-H929 | IC50 |
10.85 nM
Compound: Bortezomib
|
Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay
Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay
|
[PMID: 24767818] |
| OVCAR-3 | GI50 |
0.54 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human OVCAR3 cells
Growth inhibition of human OVCAR3 cells
|
[PMID: 24946214] |
| OVCAR-4 | GI50 |
1.95 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human OVCAR4 cells
Growth inhibition of human OVCAR4 cells
|
[PMID: 24946214] |
| OVCAR-5 | GI50 |
1.55 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human OVCAR5 cells
Growth inhibition of human OVCAR5 cells
|
[PMID: 24946214] |
| OVCAR-8 | GI50 |
2.63 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human OVCAR8 cells
Growth inhibition of human OVCAR8 cells
|
[PMID: 24946214] |
| PBMC | IC50 |
<35 nM
Compound: Bortezomib
|
Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human PBMC after 72 hrs by CellTiter-Glo luminescent cell viability assay
|
[PMID: 30365892] |
| PBMC | IC50 |
2.7 nM
Compound: 1
|
Cytotoxicity against human PBMC cells assessed as reduction in cell viability by CellTiter Glo assay
Cytotoxicity against human PBMC cells assessed as reduction in cell viability by CellTiter Glo assay
|
[PMID: 31283222] |
| PC-3 | IC50 |
7 nM
Compound: bortezomib
|
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| PC-3 | IC50 |
8.3 nM
Compound: bortezomib
|
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| PC-3 | GI50 |
2.63 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human PC3 cells
Growth inhibition of human PC3 cells
|
[PMID: 24946214] |
| PC-3 | GI50 |
0.04 μM
Compound: Bortezomib
|
Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
|
[PMID: 30802730] |
| RAW264.7 | IC50 |
0.03 μM
Compound: Bortezomib
|
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of TNFalpha-stimulated NF-kappaB activation by luciferase assay
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of TNFalpha-stimulated NF-kappaB activation by luciferase assay
|
[PMID: 32738985] |
| RKO | IC50 |
20.8 nM
Compound: Bortezomib
|
Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| RPMI-8226 | IC50 |
0.0088 μM
Compound: 3
|
Cytotoxicity against human RPMI8226 cells
Cytotoxicity against human RPMI8226 cells
|
[PMID: 20727746] |
| RPMI-8226 | IC50 |
9.5 nM
Compound: PS-341, Bortezomib
|
Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay
Cytotoxicity against human RPMI8226 cells after 48 to 72 hrs by SRB assay
|
[PMID: 24119559] |
| RPMI-8226 | IC50 |
7.96 nM
Compound: Bortezomib
|
Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay
Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay
|
[PMID: 24767818] |
| RPMI-8226 | GI50 |
0.23 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human RPMI8226 cells
Growth inhibition of human RPMI8226 cells
|
[PMID: 24946214] |
| RPMI-8226 | IC50 |
3.88 nM
Compound: Bortezomib
|
Cytotoxicity against human RPMI8226 cells after 72 hrs by MTS assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by MTS assay
|
[PMID: 26965867] |
| RPMI-8226 | IC50 |
6.7 nM
Compound: Bortezomib
|
Antiproliferative activity against human RPMI8226 cells after 72 hrs by SRB assay
Antiproliferative activity against human RPMI8226 cells after 72 hrs by SRB assay
|
[PMID: 28182990] |
| RPMI-8226 | IC50 |
11.2 nM
Compound: Bortezomib
|
Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human RPMI8226 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 29934218] |
| RPMI-8226 | IC50 |
1.43 nM
Compound: PS-341
|
Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human RPMI8226 cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| RPMI-8226 | IC50 |
0.0064 μM
Compound: BTZ
|
Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay
Antiproliferative activity against human RPMI-8226 cells cultured as 3D-spheroids assessed as reduction in cell viability after 48 hrs by Celltiter-Glo assay
|
[PMID: 34445874] |
| RPMI-8226 | IC50 |
4.7 nM
Compound: BTZ
|
Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay
Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability incubated for 72 hrs by XTT assay
|
[PMID: 34445874] |
| RPMI-8226 | IC50 |
0.0045 μM
Compound: Bortezomib
|
Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability measured after 72 hrs by XTT assay
Antiproliferative activity against human RPMI 8226 cells assessed as reduction in cell viability measured after 72 hrs by XTT assay
|
[PMID: 34969245] |
| RPMI-8226 | IC50 |
0.0056 μM
Compound: Bortezomib
|
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by XTT assay
|
[PMID: 36512676] |
| RPMI-8226 | EC50 |
0.004 μM
Compound: BTZ
|
Cytotoxicity against human RPMI-8226 cells after 72 hrs by celltitre-glo assay
Cytotoxicity against human RPMI-8226 cells after 72 hrs by celltitre-glo assay
|
[PMID: 36608337] |
| RPMI-8226 | IC50 |
5.24 μM
Compound: Bortezomib
|
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
|
[PMID: 38381886] |
| RPMI-8226 | IC50 |
80 nM
Compound: Bortezomib
|
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin assay
|
[PMID: 38381886] |
| RXF 393 | GI50 |
0.71 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human RXF393 cells
Growth inhibition of human RXF393 cells
|
[PMID: 24946214] |
| SF-268 | GI50 |
1.17 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SF268 cells
Growth inhibition of human SF268 cells
|
[PMID: 24946214] |
| SF-295 | GI50 |
1.7 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SF295 cells
Growth inhibition of human SF295 cells
|
[PMID: 24946214] |
| SF-539 | GI50 |
0.59 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SF539 cells
Growth inhibition of human SF539 cells
|
[PMID: 24946214] |
| SK-MEL-2 | GI50 |
1.07 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SK-MEL-2 cells
Growth inhibition of human SK-MEL-2 cells
|
[PMID: 24946214] |
| SK-MEL-28 | GI50 |
0.46 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SK-MEL-28 cells
Growth inhibition of human SK-MEL-28 cells
|
[PMID: 24946214] |
| SK-MEL-5 | GI50 |
0.68 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SK-MEL-5 cells
Growth inhibition of human SK-MEL-5 cells
|
[PMID: 24946214] |
| SK-OV-3 | IC50 |
130 nM
Compound: bortezomib
|
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| SK-OV-3 | IC50 |
151 nM
Compound: bortezomib
|
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| SK-OV-3 | IC50 |
66.8 nM
Compound: bortezomib
|
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKOV3 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| SK-OV-3 | GI50 |
13.8 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SKOV3 cells
Growth inhibition of human SKOV3 cells
|
[PMID: 24946214] |
| SK-OV-3 | IC50 |
1.62 nM
Compound: PS-341
|
Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay
Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| SK-OV-3 | IC50 |
12.9 nM
Compound: Bortezomib
|
Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 4 days by CellTiter-Glo assay
Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 4 days by CellTiter-Glo assay
|
[PMID: 29767973] |
| SN12C | GI50 |
1.1 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SN12C cells
Growth inhibition of human SN12C cells
|
[PMID: 24946214] |
| SNB-19 | GI50 |
2.04 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SNB19 cells
Growth inhibition of human SNB19 cells
|
[PMID: 24946214] |
| SNB-75 | GI50 |
2.04 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SNB75 cells
Growth inhibition of human SNB75 cells
|
[PMID: 24946214] |
| SR | GI50 |
0.85 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SR cells
Growth inhibition of human SR cells
|
[PMID: 24946214] |
| SW1990 | IC50 |
79.06 nM
Compound: PS-341
|
Antiproliferative activity against human SW1990 cells after 72 hrs by MTT assay
Antiproliferative activity against human SW1990 cells after 72 hrs by MTT assay
|
[PMID: 27769033] |
| SW480 | IC50 |
50 nM
Compound: bortezomib
|
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| SW480 | IC50 |
6.1 nM
Compound: bortezomib
|
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| SW480 | IC50 |
12.3 nM
Compound: bortezomib
|
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
Cytotoxicity against human SW480 cells after 72 hrs by MTT assay
|
[PMID: 21077681] |
| SW-620 | GI50 |
0.55 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human SW620 cells
Growth inhibition of human SW620 cells
|
[PMID: 24946214] |
| T47D | GI50 |
0.6 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human T47D cells
Growth inhibition of human T47D cells
|
[PMID: 24946214] |
| THP-1 | IC50 |
6.28 nM
Compound: BTZ
|
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 37979441] |
| TK-10 | GI50 |
1 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human TK10 cells
Growth inhibition of human TK10 cells
|
[PMID: 24946214] |
| TOV21G | IC50 |
16.7 nM
Compound: Bortezomib
|
Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay
Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay
|
[PMID: 26231162] |
| U-251 | GI50 |
1.55 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human U251 cells
Growth inhibition of human U251 cells
|
[PMID: 24946214] |
| U-266 | IC50 |
2.45 nM
Compound: bortezomib
|
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
|
[PMID: 19537716] |
| U-266 | IC50 |
12.2 nM
Compound: Bortezomib
|
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
|
[PMID: 19747832] |
| U-266 | IC50 |
8.8 nM
Compound: bortezomib
|
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
Cytotoxicity against human U266 cells after 72 hrs by MTT assay
|
[PMID: 20158184] |
| U-266 | IC50 |
5.73 nM
Compound: Bortezomib
|
Cytotoxicity against human U266 cells after 72 hrs by MTS assay
Cytotoxicity against human U266 cells after 72 hrs by MTS assay
|
[PMID: 26965867] |
| U-266 | GI50 |
0.001 μM
Compound: Bortezomib
|
Antiproliferative activity against human U266 cells after 72 hrs by calcein AM staining based fluorescence assay
Antiproliferative activity against human U266 cells after 72 hrs by calcein AM staining based fluorescence assay
|
[PMID: 28441582] |
| U-266 | IC50 |
11.63 nM
Compound: Bortezomib
|
Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
Cytotoxicity against human U266B1 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 29934218] |
| U-266 | IC50 |
12.5 nM
Compound: PS-341
|
Antiproliferative activity against human U266 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human U266 cells incubated for 48 hrs by MTT assay
|
[PMID: 32267687] |
| U-87MG ATCC | IC50 |
7.86 μM
Compound: Bortezomib
|
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
Cytotoxicity against human U87 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin assay
|
[PMID: 38381886] |
| UACC-257 | GI50 |
0.59 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human UACC257 cells
Growth inhibition of human UACC257 cells
|
[PMID: 24946214] |
| UACC-62 | GI50 |
0.91 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human UACC62 cells
Growth inhibition of human UACC62 cells
|
[PMID: 24946214] |
| UO-31 | GI50 |
1.05 nM
Compound: Bortezomib, Velcade
|
Growth inhibition of human UO31 cells
Growth inhibition of human UO31 cells
|
[PMID: 24946214] |
| WM 266-4 | IC50 |
0.035 μM
Compound: Bortezomib, Velcade, PS-341
|
Cytotoxicity against human WM266.4 cells after 72 hrs by ATPlite assay
Cytotoxicity against human WM266.4 cells after 72 hrs by ATPlite assay
|
[PMID: 22206869] |
Bortezomib (PS-341) (100 nM; 8 hours) results in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1[1].
Bortezomib (PS-341) (5-100 nM; 20 hours) induces apoptosis in mantle-cell lymphoma (MCL) cell lines[3].
Bortezomib (PS-341) (20 nM; 1-14 hours) induces Noxa up-regulation in both MCL cell lines[3].
The IC50 of Bortezomib (PS-341) is found to be 2.46 nM for 26S proteasome in the B16F10 cells[4].
Bortezomib (PS-341) suppresses several anti-apoptotic proteins (e.g., Bcl-XL, Bcl-2, and STAT-3)[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:PC-3 cells
-
Concentration:100 nM
-
Incubation Time:8 hours
-
Result:Resulted in the accumulation of cells in G2-M, with a corresponding decrease in the number of cells in G1.
-
Cell Line:JVM-2, Granta-519, Jeko, REC-1 cells (MCL cell lines)
-
Concentration:5-100 nM
-
Incubation Time:20 hours
-
Result:The median LD50 for these MCL cell lines was 31 nM (range, 18.2-60.1 nM).
-
Cell Line:wtp53 (Granta-519), mutp53 (Jeko) cells
-
Concentration:20 nM
-
Incubation Time:1, 2, 4, 6, 14 hours
-
Result:Noxa up-regulation was detected between 2 to 4 hours after bortezomib (PS-341).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male nude mice (xenograft tumor model bearing PC-3 cells)[1]
-
Dosage:0.3, 1 mg/kg
-
Administration:Intravenous injection; once weekly for 4 weeks
-
Result:Resulted in a significant decrease in tumor growth ~60% at dose of 1 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 179324-69-7
-
Appearance Solid
-
Molecular Weight 384.24
-
Formel C19H25BN4O4
-
Color White to off-white
-
SMILES
OB(O)[C@H](CC(C)C)NC([C@@H](NC(C1=NC=CN=C1)=O)CC2=CC=CC=C2)=O
-
Synonyms
PS-341; LDP-341; NSC 681239
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (261)
-
Journal Impact Factor
-
Most Recent
-
Signal Transduct Target Ther
Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]2025 Dec 15;10(1):406. PMID: 41392286 -
Signal Transduct Target Ther
Glucosidase alpha neutral C promotes influenza virus replication by inhibiting proteosome-dependent degradation of hemagglutinin. [Abstract]2025 Apr 23;10(1):131. PMID: 40263249 -
Nature
2026 Jan;649(8096):477-486. PMID: 41193799 -
Cell
2019 Jul 11;178(2):330-345.e22. PMID: 31257027 -
Cancer Discov
Divergent Evolution of Malignant Subclones Maintains a Balance Between Induced Aggressiveness and Intrinsic Drug Resistance in T Cell Cancer. [Abstract]2025 Jun 16. PMID: 40516109 -
Nat Cancer
Discovering the anti-cancer potential of non-oncology drugs by systematic viability profiling. [Abstract]2020 Feb;1(2):235-248. PMID: 32613204 -
Nat Immunol
An epithelial cell-derived metabolite tunes immunoglobulin A secretion by gut-resident plasma cells. [Abstract]2023 Mar;24(3):531-544. PMID: 36658240 -
Cell Res
2026 Mar;36(3):219-232. PMID: 41634384 -
Cancer Commun (Lond)
Orchestrated desaturation reprogramming from stearoyl-CoA desaturase to fatty acid desaturase 2 in cancer epithelial-mesenchymal transition and metastasis. [Abstract]2025 Mar;45(3):245-280. PMID: 39722173 -
Drug Resist Updat
NDRG1 overcomes resistance to immunotherapy of pancreatic ductal adenocarcinoma through inhibiting ATG9A-dependent degradation of MHC-1. [Abstract]2024 Mar:73:101040. PMID: 38228036 -
Nat Commun
2026 May 30. PMID: 42218123 -
Nat Commun
Multiple myeloma associated long non-coding RNA PLUM confers chemoresistance by enhancing PRC2 mediated UPR pathway activation. [Abstract]2025 Sep 1;16(1):8155. PMID: 40890111 -
Nat Commun
Small round cell sarcoma tumoroid biobank reveals CIC::DUX4 sarcoma vulnerability to MCL-1 inhibition. [Abstract]2025 Aug 21;16(1):7689. PMID: 40841360 -
Nat Commun
A mouse protozoan boosts antigen-specific mucosal IgA responses in a specific lipid metabolism- and signaling-dependent manner. [Abstract]2024 Sep 10;15(1):7914. PMID: 39256385 -
Nat Commun
Super enhancer acquisition drives expression of oncogenic PPP1R15B that regulates protein homeostasis in multiple myeloma. [Abstract]2024 Aug 9;15(1):6810. PMID: 39122682 -
Nat Commun
FBXO7 ubiquitinates PRMT1 to suppress serine synthesis and tumor growth in hepatocellular carcinoma. [Abstract]2024 Jun 5;15(1):4790. PMID: 38839752 -
Nat Commun
2023 Nov 23;14(1):7656. PMID: 37996419 -
Nat Commun
Exploiting endogenous and therapy-induced apoptotic vulnerabilities in immunoglobulin light chain amyloidosis with BH3 mimetics. [Abstract]2022 Oct 2;13(1):5789. PMID: 36184661 -
Nat Commun
The ubiquitylation of IL-1β limits its cleavage by caspase-1 and targets it for proteasomal degradation. [Abstract]2021 May 11;12(1):2713. PMID: 33976225 -
Nat Commun
Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]2020 Sep 4;11(1):4417. PMID: 32887884 -
Nat Commun
pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase. [Abstract]2017 May 22;8:15398. PMID: 28530236 -
Cell Death Differ
TRIM3 facilitates ferroptosis in non-small cell lung cancer through promoting SLC7A11/xCT K11-linked ubiquitination and degradation. [Abstract]2024 Jan;31(1):53-64. PMID: 37978273 -
Acta Pharm Sin B
2024 Dec;14(12):5382-5392. PMID: 39807332 -
Acta Pharm Sin B
Phenylalanine deprivation inhibits multiple myeloma progression by perturbing endoplasmic reticulum homeostasis. [Abstract]2024 Aug;14(8):3493-3512. PMID: 39220878 -
Acta Pharm Sin B
Chemical screen identifies shikonin as a broad DNA damage response inhibitor that enhances chemotherapy through inhibiting ATM and ATR. [Abstract]2022 Mar;12(3):1339-1350. PMID: 35530159 -
Hemasphere
Novel Peptide-drug Conjugate Melflufen Efficiently Eradicates Bortezomib-resistant Multiple Myeloma Cells Including Tumor-initiating Myeloma Progenitor Cells. [Abstract]2021 Jun 12;5(7):e602. PMID: 34136753 -
-
Adv Sci (Weinh)
Targeting PRKCN, an Essential Driver Orchestrating mTOR-IRF4 Axis Independently of Kinase Activity, in Multiple Myeloma. [Abstract]2026 Apr;13(21):e18975. PMID: 41655233 -
Adv Sci (Weinh)
TRIM47 Regulates Energy Metabolism via Glycolytic Reprogramming to Drive Hepatocellular Carcinoma Progression and Represents an Efficient Therapeutic Target. [Abstract]2026 Mar;13(17):e16996. PMID: 41632101 -
Adv Sci (Weinh)
OTUD6A in Airway Epithelial Cells Exacerbates Allergic Asthma by Promoting Airway Inflammation and Airway Remodeling Through Deubiquitination of hResistin/mRELMα. [Abstract]2026 Jan 20:e16355. PMID: 41560298 -
Adv Sci (Weinh)
NADH-Reductive Stress Induced by Dihydrolipoamide Dehydrogenase Activation Contributes to Cuproptosis. [Abstract]2025 Dec 5:e20444. PMID: 41346305 -
Adv Sci (Weinh)
The Crosstalk Between CRL5 and APC/C E3 Ligases Regulates Metastasis and Chemosensitivity of Cancer Cells. [Abstract]2025 Oct 29:e12652. PMID: 41159544 -
Adv Sci (Weinh)
Palmitoyltransferase ZDHHC3 Aggravates Nonalcoholic Steatohepatitis by Targeting S-Palmitoylated IRHOM2. [Abstract]2023 Oct;10(28):e2302130. PMID: 37544908 -
Leukemia
Human gene-engineered calreticulin mutant stem cells recapitulate MPN hallmarks and identify targetable vulnerabilities. [Abstract]2023 Apr;37(4):843-853. PMID: 36813992 -
Theranostics
ATF4 destabilizes RET through nonclassical GRP78 inhibition to enhance chemosensitivity to bortezomib in human osteosarcoma. [Abstract]2019 Aug 14;9(21):6334-6353. PMID: 31534554 -
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J Exp Clin Cancer Res
OTULIN confers cisplatin resistance in osteosarcoma by mediating GPX4 protein homeostasis to evade the mitochondrial apoptotic pathway. [Abstract]2024 Dec 26;43(1):330. PMID: 39721999 -
Cell Discov
2025 Sep 30;11(1):80. PMID: 41027888 -
Plant Commun
Phosphorylation of PIP2;7 by CPK28 or Phytophthora kinase effectors dampens pattern-triggered immunity in Arabidopsis. [Abstract]2024 Sep 13:101135. PMID: 39277790 -
J Control Release
Immunogenic cell death-primed autophagosome vaccines drive dendritic cell cross-presentation and suppress colon cancer metastasis. [Abstract]2026 May 10:393:114827. PMID: 41856327 -
J Hazard Mater
Di-(2-ethylhexyl) phthalate (DEHP) and its metabolite promote multiple myeloma progression and bortezomib resistance. [Abstract]2025 Sep 5:495:139147. PMID: 40633344 -
J Hazard Mater
2024 Jul 31:477:135391. PMID: 39106724 -
Gut Microbes
IgA-mediated control of host-microbial interaction during weaning reaction influences gut inflammation. [Abstract]2024 Jan-Dec;16(1):2323220. PMID: 38439579 -
EBioMedicine
VIPAS39 confers ferroptosis resistance in epithelial ovarian cancer through exporting ACSL4. [Abstract]2025 Apr:114:105646. PMID: 40088627 -
J Immunother Cancer
HSP47 inhibition-induced CD155 expression through TRAF2 deubiquitination promotes tumor immune evasion. [Abstract]2025 Nov 28;13(11):e011976. PMID: 41314980 -
Cell Rep Med
Augment proteasome inhibitor efficacy activates CD8+ T cell-mediated antitumor immunity in breast cancer. [Abstract]2025 Jul 15;6(7):102211. PMID: 40609539 -
Cell Rep Med
CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]2025 Apr 2:102053. PMID: 40187357 -
Clin Cancer Res
A Novel mTORC1/2 Inhibitor (MTI-31) Inhibits Tumor Growth, Epithelial-Mesenchymal Transition, Metastases, and Improves Antitumor Immunity in Preclinical Models of Lung Cancer. [Abstract]2019 Jun 15;25(12):3630-3642. PMID: 30796032
Bortezomib purchased from MedChemExpress. Usage Cited in: Clin Cancer Res. 2019 Jun 15;25(12):3630-3642. [Abstract]
H1975 cells treated with 5 μmol/L MTI-31 alone or in combination with 10 μmol/L CQ or 0.01 μmol/L PS-341.
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Nat Struct Mol Biol
2025 Jun 24. PMID: 40555785 -
Cancer Lett
DUSP2 recruits CSNK2A1 to suppress AKT1-mediated apoptosis resistance under hypoxic microenvironment in pancreatic cancer. [Abstract]2023 Aug 1:568:216288. PMID: 37390887 -
Cancer Lett
LncRNA MNX1-AS1 sustains inactivation of Hippo pathway through a positive feedback loop with USP16/IGF2BP3 axis in gallbladder cancer. [Abstract]2022 Oct 28:547:215862. PMID: 35953000 -
Cancer Lett
All-trans retinoic acid exerts selective anti-FLT3-ITD acute myeloid leukemia efficacy through downregulating Chk1 kinase. [Abstract]2020 Mar 31;473:130-138. PMID: 31904486 -
Cell Death Dis
Targeting PPARγ via SIAH1/2-mediated ubiquitin-proteasomal degradation as a new therapeutic approach in luminal-type bladder cancer. [Abstract]2024 Dec 18;15(12):908. PMID: 39695138 -
Cell Death Dis
PRMT1 methylation of WTAP promotes multiple myeloma tumorigenesis by activating oxidative phosphorylation via m6A modification of NDUFS6. [Abstract]2023 Aug 9;14(8):512. PMID: 37558663 -
Cell Death Dis
Targeted inhibition of protein synthesis renders cancer cells vulnerable to apoptosis by unfolded protein response. [Abstract]2023 Aug 26;14(8):561. PMID: 37626037 -
Cell Death Dis
PP6 negatively modulates LUBAC-mediated M1-ubiquitination of RIPK1 and c-FLIPL to promote TNFα-mediated cell death. [Abstract]2022 Sep 7;13(9):773. PMID: 36071040 -
Cell Death Dis
ΔNp63α promotes Bortezomib resistance via the CYGB-ROS axis in head and neck squamous cell carcinoma. [Abstract]2022 Apr 9;13(4):327. PMID: 35397613 -
Cell Death Dis
2022 May 12;13(5):451. PMID: 35551175 -
Cell Death Dis
2022 Feb 10;13(2):136. PMID: 35145058 -
Cell Death Dis
TRIB2 modulates proteasome function to reduce ubiquitin stability and protect liver cancer cells against oxidative stress. [Abstract]2021 Jan 7;12(1):42. PMID: 33414446 -
Cell Death Dis
The proton pump inhibitor pantoprazole disrupts protein degradation systems and sensitizes cancer cells to death under various stresses. [Abstract]2018 May 22;9(6):604. PMID: 29789637
Bortezomib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604. [Abstract]
The accumulated SQSTM1 by either proteasome inhibitors or PPI was sensitive to autophagy mediated degradation. AGS cells were pretreated with 25 and 50nM bortezomib for 1h, and then incubated with 500nM torin 1 for 24h (g). After pretreatment with PPI for 24h in pH 7.4 or pH 6.5 condition, rapamycin (1μM) or torin 1 (500 nM) was added for another 24h (h). The protein level of SQSTM1 was measured by western blot analysis (g, h).
Bortezomib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604. [Abstract]
Different concentrations of two classical proteasome inhibitors Bortezomib and MG132 are added. AGS cells are either untreated or treated with Bortezomib (25 nM) or MG132 (0.1 μM) for 24 h in the absence or presence of baf A1 (100 nM).
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Proc Natl Acad Sci U S A
Activation of the NLRP1 inflammasome in human keratinocytes by the dsDNA mimetic poly(dA:dT). [Abstract]2023 Jan 31;120(5):e2213777120. PMID: 36693106 -
Proc Natl Acad Sci U S A
2022 Nov;119(44):e2214227119. PMID: 36279464 -
Cell Commun Signal
MIR4726EccDNA drives bortezomib resistance in multiple myeloma by enhancing MIR4726-5p/NXF1/NKIRAS2 axis dependent autophagy. [Abstract]2025 Jul 18;23(1):346. PMID: 40682103 -
Cell Commun Signal
2025 Jan 28;23(1):53. PMID: 39875995 -
Dev Cell
Lactylation of LSD1 is an acquired epigenetic vulnerability of BRAFi/MEKi-resistant melanoma. [Abstract]2025 Mar 20:S1534-5807(25)00121-2. PMID: 40132584 -
Int J Biol Macromol
Identification of c.146G > A mutation in a Fabry patient and its correction by customized Cas9 base editors in vitro. [Abstract]2024 Oct 25:136922. PMID: 39490876 -
Acta Pharmacol Sin
2025 Mar 25. PMID: 40133626 -
Acta Pharmacol Sin
Inhibition of CDC27 O-GlcNAcylation coordinates the antitumor efficacy in multiple myeloma through the autophagy-lysosome pathway. [Abstract]2025 Jul;46(7):2041-2055. PMID: 39984622 -
Acta Pharmacol Sin
2019 Sep;40(9):1245-1255. PMID: 31138898 -
EMBO J
Tyrosine kinase targeting uncovers oncogenic pathway plasticity in Tasmanian devil transmissible cancers. [Abstract]2025 Nov 3. PMID: 41184587 -
Phytomedicine
Columbianadin targets TRIM7 to maintain P2X7 palmitoylation, inhibiting cuproptosis in synovial M2 macrophages. [Abstract]2025 Oct:146:157091. PMID: 40768810 -
EMBO J
Interferon-induced PARP14-mediated ADP-ribosylation in p62 bodies requires the ubiquitin-proteasome system. [Abstract]2025 Apr 7. PMID: 40195501 -
EMBO J
E3 ubiquitin ligase CHIP facilitates cAMP and cGMP signalling cross-talk by polyubiquitinating PDE9A. [Abstract]2025 Feb;44(4):1249-1273. PMID: 39806097 -
Phytomedicine
Ethanol extract of Eclipta prostrata induces multiple myeloma ferroptosis via Keap1/Nrf2/HO-1 axis. [Abstract]2024 Jun:128:155401. PMID: 38507850 -
Phytomedicine
Sculponeatin A promotes the ETS1-SYVN1 interaction to induce SLC7A11/xCT-dependent ferroptosis in breast cancer. [Abstract]2023 Aug:117:154921. PMID: 37327642 -
Free Radic Biol Med
Targeting ABCB6 with nitidine chloride inhibits PI3K/AKT signaling pathway to promote ferroptosis in multiple myeloma. [Abstract]2023 Jul:203:86-101. PMID: 37044150 -
Chemosphere
Bisphenol C induces developmental defects in liver and intestine through mTOR signaling in zebrafish (Danio rerio). [Abstract]2023 May:322:138195. PMID: 36822516 -
New Phytol
An F-box protein attenuates fungal xylanase-triggered immunity by destabilizing LRR-RLP NbEIX2 in a SOBIR1-dependent manner. [Abstract]2022 Dec;236(6):2202-2215. PMID: 36151918 -
NPJ Precis Oncol
Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]2025 Nov 21;9(1):373. PMID: 41272086 -
Clin Sci
LONP1 facilitates pulmonary artery smooth muscle cell glycolytic reprogramming by degrading MPC1 in pulmonary hypertension. [Abstract]2025 May 7:CS20255922. PMID: 40332105 -
Br J Pharmacol
Sculponeatin A induces mitochondrial dysfunction in non-small cell lung cancer through WWP2-mediated degradation of mitochondrial STAT3. [Abstract]2025 Jun;182(12):2662-2681. PMID: 39993792 -
Br J Pharmacol
A novel sorbicillinoid compound as a potent anti-inflammation agent through inducing NLRP3 protein degradation. [Abstract]2023 Aug;180(15):1930-1948. PMID: 36788033 -
NPJ Breast Cancer
Clonal heterogeneity in ER+ breast cancer reveals the proteasome and PKC as potential therapeutic targets. [Abstract]2023 Dec 2;9(1):97. PMID: 38042915 -
J Transl Med
CBX7 regulates chemotherapy-induced senescence-like growth arrest in multiple myeloma via the ERK/STAT3/PIM1 axis. [Abstract]2025 Nov 17;23(1):1292. PMID: 41250171 -
J Transl Med
Single-cell transcriptomics identifies PDIA4 as a marker of progression and therapeutic vulnerability in multiple myeloma. [Abstract]2025 Oct 21;23(1):1136. PMID: 41121130 -
J Transl Med
Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis. [Abstract]2024 Dec 3;22(1):1095. PMID: 39623468 -
Curr Biol
UBP12 and UBP13 deubiquitinases destabilize the CRY2 blue light receptor to regulate Arabidopsis growth. [Abstract]2022 Aug 8;32(15):3221-3231.e6. PMID: 35700731 -
Amyloid
2019 Mar;26(1):24-33. PMID: 30739503 -
Oncogene
Melatonin potentiates the cytotoxic effect of Neratinib in HER2+ breast cancer through promoting endocytosis and lysosomal degradation of HER2. [Abstract]2021 Nov;40(44):6273-6283. PMID: 34556812 -
Cell Chem Biol
2022 Oct 20;29(10):1470-1481.e31. PMID: 36070758 -
Blood Adv
BH3 mimetic drugs overcome the microenvironment-induced resistance to crizotinib in ALK+ anaplastic large cell lymphoma. [Abstract]2025 Jul 2:bloodadvances.2024015322. PMID: 40601898 -
Cell Death Discov
ChaC1-based drug screenings identify a synergistic lethal effect of auranofin and proteasome inhibitors in hepatocellular carcinoma cells. [Abstract]2025 Nov 17;11(1):532. PMID: 41249117 -
Cell Death Discov
YAP ISGylation increases its stability and promotes its positive regulation on PPP by stimulating 6PGL transcription. [Abstract]2022 Feb 11;8(1):59. PMID: 35149670 -
Cell Rep
The Hippo pathway kinase MST1 mediates a feedback loop to maintain NLRP3 inflammasome homeostasis. [Abstract]2025 Jul 26;44(8):116076. PMID: 40716062 -
Cell Rep
The N-degron pathway mediates the autophagic degradation of cytosolic mitochondrial DNA during sterile innate immune responses. [Abstract]2024 Dec 21;44(1):115094. PMID: 39709605 -
Cell Rep
Deciphering ER stress-unfolded protein response relationship by visualizing unfolded proteins in the ER. [Abstract]2024 Jun 11;43(6):114358. PMID: 38865243 -
Cell Rep
The molecular network of the proteasome machinery inhibition response is orchestrated by HSP70, revealing vulnerabilities in cancer cells. [Abstract]2022 Sep 27;40(13):111428. PMID: 36170818 -
Cell Rep
The Zscan4-Tet2 Transcription Nexus Regulates Metabolic Rewiring and Enhances Proteostasis to Promote Reprogramming. [Abstract]2020 Jul 14;32(2):107877. PMID: 32668244 -
J Med Chem
Discovery and Characterization of a First-In-Class HCK/BTK PROTAC DFCI-002-06 for the Treatment of MYD88 Mutated B Cell Malignancies. [Abstract]2026 Jan 22;69(2):1119-1134. PMID: 41482966 -
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
2023 Dec 28;66(24):16597-16614. PMID: 38088921 -
Sci Signal
Degradation of HDAC10 by autophagy promotes IRF3-mediated antiviral innate immune responses. [Abstract]2022 Dec 20;15(765):eabo4356. PMID: 36538592 -
J Cell Biol
2025 Mar 3;224(3):e202404084. PMID: 39786340 -
Elife
Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome. [Abstract]2018 Aug 1;7:e38430. PMID: 30067223
Bortezomib purchased from MedChemExpress. Usage Cited in: Elife. 2018 Aug 1;7:e38430. [Abstract]
Kelly cells are treated with increasing concentrations of Thalidomide and co-treated with 5 μM Bortezomib, 5 μM MLN4924, 0.5 μM MLN7243, or DMSO as a control. Following 24 h incubation, SALL4 and GAPDH protein levels are assessed by western blot analysis.
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J Agric Food Chem
Isolation, Identification, and Immunomodulatory Mechanism of Peptides from Lepidium meyenii (Maca) Protein Hydrolysate. [Abstract]2022 Apr 13;70(14):4328-4341. PMID: 35357828 -
J Agric Food Chem
Alpinia hainanensis Rhizome Extract Ameliorates Dextran Sulfate Sodium-Induced Ulcerative Colitis: Active Ingredient Investigation and Evaluation. [Abstract]2022 Apr 6;70(13):3989-3999. PMID: 35321548 -
Ecotoxicol Environ Saf
Phthalates promote lenvatinib resistance in hepatocellular carcinoma through the HPX-MAPK pathway. [Abstract]2025 Aug 25:303:118932. PMID: 40858030 -
JCI Insight
2023 Mar 22;8(6):e141110. PMID: 36802340 -
Eur J Med Chem
2020 Nov 15;206:112708. PMID: 32810752 -
Neurosci Bull
2025 Dec 27. PMID: 41455075 -
Int J Mol Med
Proteasome inhibitors decrease paclitaxel‑induced cell death in nasopharyngeal carcinoma with the accumulation of CDK1/cyclin B1. [Abstract]2021 Oct;48(4):193. PMID: 34435645 -
Biomater Sci
Versatile functionalization of surface-tailorable polymer nanohydrogels for drug delivery systems. [Abstract]2018 Dec 18;7(1):247-261. PMID: 30465554 -
Biochem Pharmacol
Apelin-13 improves pulmonary epithelial barrier function in a mouse model of LPS-induced acute lung injury by inhibiting Chk1-mediated DNA damage. [Abstract]2024 May 25:116297. PMID: 38801925 -
Biochem Pharmacol
2022 Oct:204:115232. PMID: 36030831 -
Mol Cancer Ther
Functional genomics and proteomics identify Folate Carrier SLC19A1 as a predictor of pralatrexate sensitivity in diverse T-cell lymphoma models. [Abstract]2026 Jun 13. PMID: 42295240 -
World J Gastroenterol
Wogonin derivative V8 enhances bortezomib efficacy in gastric carcinoma by disrupting lysosome-mediated drug resistance. [Abstract]2026 Feb 28;32(8):113299. PMID: 41809875 -
Mol Ther Oncol
The oligosaccharyltransferase complex is an essential component of multiple myeloma plasma cells. [Abstract]2025 Mar 8;33(2):200964. PMID: 40200920 -
Cells
MDM2 Drives Proteasome Inhibitor Resistance and Represents a TP53-Independent Therapeutic Vulnerability in Multiple Myeloma. [Abstract]2026 May 1;15(9):831. PMID: 42121932 -
Cells
Fragment-Sized and Bidentate (Immuno)Proteasome Inhibitors Derived from Cysteine and Threonine Targeting Warheads. [Abstract]2021 Dec 6;10(12):3431. PMID: 34943940 -
Life Sci
Melatonin ameliorates myocardial ischemia/reperfusion injury via regulating the ubiquitin-proteasome system. [Abstract]2025 Nov 1:380:123973. PMID: 40962023 -
Commun Biol
Infection with novel duck reovirus induces stress granule and methylation-mediated host translational shutoff in Muscovy ducklings. [Abstract]2024 Nov 21;7(1):1549. PMID: 39572728 -
Commun Biol
A pipeline for malignancy and therapy agnostic assessment of cancer drug response using cell mass measurements. [Abstract]2022 Nov 26;5(1):1295. PMID: 36435843 -
Stem Cell Reports
Inhibition of Farnesyltransferase Potentiates NOTCH-Targeted Therapy against Glioblastoma Stem Cells. [Abstract]2017 Dec 12;9(6):1948-1960. PMID: 29198824 -
Respir Res
SPP1 induces idiopathic pulmonary fibrosis and NSCLC progression via the PI3K/Akt/mTOR pathway. [Abstract]2024 Oct 5;25(1):362. PMID: 39369217 -
Mol Plant Pathol
Phytoplasma effector SWP1 induces witches' broom symptom by destabilizing the TCP transcription factor BRANCHED1. [Abstract]2018 Dec;19(12):2623-2634. PMID: 30047227 -
Pharmaceuticals (Basel)
The Proteasome Inhibitor Marizomib Evokes Endoplasmic Reticulum Stress and Promotes Apoptosis in Human Glioblastoma Cells. [Abstract]2024 Aug 20;17(8):1089. PMID: 39204194 -
Cell Oncol (Dordr)
Proteasomal deubiquitylase activity enhances cell surface recycling of the epidermal growth factor receptor in non-small cell lung cancer. [Abstract]2022 Oct;45(5):951-965. PMID: 36129611 -
Int J Cancer
Beneficial effects of aerobic exercises on multiple myeloma: Mechanisms and clinical observations. [Abstract]2025 Jul 4. PMID: 40613758 -
Int Immunopharmacol
2020 Mar 3;82:106259. PMID: 32143000 -
Eur J Pharmacol
Hinokitiol copper complex inhibits proteasomal deubiquitination and induces paraptosis-like cell death in human cancer cells. [Abstract]2017 Nov 15:815:147-155. PMID: 28887042
Bortezomib purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2017 Nov 15:815:147-155. [Abstract]
Shown are GFPu fluorescent images of the GFPu-HEK293 cells treated with CuSO4 (Cu, 20 μM), HK (20 μM), HK-Cu (HC, 20 μM), or Velcade (Vel, 100 nM).
-
J Med Virol
E3 ubiquitin ligase FBXO22 inhibits SARS-CoV-2 replication via promoting proteasome-dependent degradation of NSP5. [Abstract]2024 Sep;96(9):e29891. PMID: 39223933 -
Antimicrob Agents Chemother
Inhibitors of the 20S proteasome β5 subunit as potent and selective agents against Trichomonas vaginalis. [Abstract]2025 Dec 10;69(12):e0089325. PMID: 41218108 -
Mol Pharm
Using Metal-Organic Framework Nanoparticles for Targeted Codelivery of Bortezomib and Iron Ions to Mitochondrial TOM20 to Induce Ferroptosis for Colorectal Cancer Treatment. [Abstract]2025 Aug 4;22(8):4865-4878. PMID: 40671590 -
Cell Rep Methods
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]2023 Oct 23;3(10):100599. PMID: 37797618 -
Front Cell Dev Biol
2021 Mar 30:9:633259. PMID: 33859984 -
Biochim Biophys Acta Mol Basis Dis
The deubiquitinase OTUB1 governs lung cancer cell fitness by modulating proteostasis of OXPHOS proteins. [Abstract]2023 Oct;1869(7):166767. PMID: 37245529 -
FASEB J
2021 Aug;35(8):e21800. PMID: 34324733 -
J Cell Mol Med
Bortezomib suppresses self-renewal and leukemogenesis of leukemia stem cell by NF-ĸB-dependent inhibition of CDK6 in MLL-rearranged myeloid leukemia. [Abstract]2021 Mar;25(6):3124-3135. PMID: 33599085 -
iScience
An oncolytic vaccinia virus encoding CD47 nanobody potentiates antitumor immunity in multiple myeloma. [Abstract]2026 Feb 28;29(4):115174. PMID: 41858619 -
iScience
TLR9 decreases FOXO3 expression to prevent excessive inflammation in macrophage activation syndrome. [Abstract]2025 Nov 17;28(12):114098. PMID: 41438053 -
iScience
Computational design of diverse nuclear factor erythroid 2 activators with cellular antioxidative activity. [Abstract]2025 May 8;28(6):112621. PMID: 40502689 -
iScience
Dynamic regulation of P-TEFb by 7SK snRNP is integral to the DNA damage response to regulate chemotherapy sensitivity. [Abstract]2022 Aug 4;25(9):104844. PMID: 36034227 -
iScience
Identification of a drug-response gene in multiple myeloma through longitudinal single-cell transcriptome sequencing. [Abstract]2022 Jul 19;25(8):104781. PMID: 35992084 -
J Inflamm Res
Aqueous Extract of Cimicifuga dahurica Reprogramming Macrophage Polarization by Activating TLR4-NF-κB Signaling Pathway. [Abstract]2022 Feb 15;15:1027-1046. PMID: 35210810 -
Transl Oncol
poly(I:C) synergizes with proteasome inhibitors to induce apoptosis in cervical cancer cells. [Abstract]2022 Apr;18:101362. PMID: 35151092 -
J Cell Physiol
2025 Jan;240(1):e31459. PMID: 39373061 -
Virol Sin
Proteasome Inhibitor PS-341 Effectively Blocks Infection by the Severe Fever with Thrombocytopenia Syndrome Virus. [Abstract]2019 Oct;34(5):572-582. PMID: 31637631 -
J Biol Chem
Andrographolide targets syndecan4 to impair its interaction with syntenin and inhibits the biogenesis of small extracellular vesicles. [Abstract]2026 Jan 20:111182. PMID: 41570990 -
Sci Rep
NPS-2143 suppresses malignant phenotypes of retinoblastoma cells involved in regulating NF-κB pathway. [Abstract]2025 May 9;15(1):16209. PMID: 40346093 -
Sci Rep
Elucidating host cell response pathways and repurposing therapeutics for SARS-CoV-2 and other coronaviruses. [Abstract]2022 Nov 5;12(1):18811. PMID: 36335206 -
Aging
Cardamonin induces G2/M phase arrest and apoptosis through inhibition of NF-κB and mTOR pathways in ovarian cancer. [Abstract]2020 Nov 25;12(24):25730-25743. PMID: 33234722 -
J Virol
SUMOylation-dependent degradation of nucleocapsid is responsible for Pestivirus uncoating. [Abstract]2025 Nov 25:e0164825. PMID: 41288382 -
Chem Res Toxicol
The Selective SIRT3 Inhibitor 3-TYP Represses Primary Myeloma Growth by Reducing c-Myc Stability. [Abstract]2024 Jun 17;37(6):1062-1069. PMID: 38815162 -
J Virol
ATF6-Mediated Unfolded Protein Response Facilitates Adeno-associated Virus 2 (AAV2) Transduction by Releasing the Suppression of the AAV Receptor on Endoplasmic Reticulum Stress. [Abstract]2022 Feb 9;96(3):e0110321. PMID: 34851146 -
Cell Signal
PERK-eIF2alpha-mediated translational inhibition of MCL-1 contributes to potential 2-deoxy-D-glucose and BAD mimetic combinatorial cancer therapy. [Abstract]2025 Dec 19:139:112333. PMID: 41423011 -
J Photochem Photobiol B
Suppression of NRF2 by photodynamic action to enhance bortezomib-triggered DNA damage for synergistic colorectal cancer therapy. [Abstract]2025 Apr 3:267:113162. PMID: 40199069 -
Cell Signal
Identification of a new micropeptide altKLF4 derived from KLF4 that influences myeloma chemotherapeutic sensitivity. [Abstract]2025 Mar 25:111767. PMID: 40147548 -
Cell Signal
tRNA methyltransferase DNMT2 promotes hepatocellular carcinoma progression and enhances Bortezomib resistance through inhibiting TNFSF10. [Abstract]2024 Nov 29:127:111533. PMID: 39617358 -
Mol Cell Biochem
A novel 2-iminobenzimidazole compound, XYA1353, displays in vitro and in vivo anti-myeloma activity via targeting NF-κB signaling. [Abstract]2024 Apr;479(4):843-857. PMID: 37204666
Bortezomib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2024 Apr;479(4):843-857. [Abstract]
Bortezomib (BTZ; 5, 10, 20 nM; 48 h) increases the expression level of γH2AX in RPMI-8226 and U266 cells.
Bortezomib purchased from MedChemExpress. Usage Cited in: Mol Cell Biochem. 2024 Apr;479(4):843-857. [Abstract]
Bortezomib (BTZ; 10 nM; 48 h) significantly enhances the cell death of RPMI-8226.
-
Proteomes
Azidohomoalanine (AHA) Metabolic Labeling Reveals Unique Proteomic Insights into Protein Synthesis and Degradation in Response to Bortezomib Treatment. [Abstract]2025 Nov 25;13(4):63. PMID: 41441334 -
Heliyon
2023 Feb 1;9(2):e13397. PMID: 36846655 -
Epigenomes
2026 Feb 23;10(1):14. PMID: 41892363 -
Exp Cell Res
KLF15-activated MARCH2 boosts cell proliferation and epithelial-mesenchymal transition and presents diagnostic significance for hepatocellular carcinoma. [Abstract]2024 Jun 5:114117. PMID: 38848952 -
Exp Cell Res
2023 Sep 15;430(2):113718. PMID: 37468057 -
Med Oncol
Proteasome inhibitors attenuates mitoxantrone-triggered immunogenic cell death in prostate cancer cells. [Abstract]2020 Nov 19;37(12):116. PMID: 33215275 -
Exp Cell Res
Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]2020 Aug 1;393(1):112054. PMID: 32376287 -
ChemMedChem
Synthesis of Novel d-Glucopyranuronamide-Based Nucleos(t)ide Analogs Bearing (Triazolyl)methyl Phosph(on)ate Motifs With Anticancer and Antibacterial Potential. [Abstract]2026 Jun 26;21(12):e70328. PMID: 42315993 -
J Immunol
Duck MARCH8 Negatively Regulates the RLR Signaling Pathway through K29-Linked Polyubiquitination of MAVS. [Abstract]2023 Mar 15;210(6):786-794. PMID: 36715497 -
BMC Cancer
Bortezomib potentiates antitumor activity of mitoxantrone through dampening Wnt/β-catenin signal pathway in prostate cancer cells. [Abstract]2021 Oct 13;21(1):1101. PMID: 34645397 -
PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351 -
BMC Cancer
Post-transcriptional regulation of cancer/testis antigen MAGEC2 expression by TRIM28 in tumor cells. [Abstract]2018 Oct 11;18(1):971. PMID: 30309319
Bortezomib purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2018 Oct 11;18(1):971. [Abstract]
The reduction of MAGEC2 protein level in TRIM28-knockdown A375 cells can be inhibited by treatment with both MG132 and PS-341, and similar result is also observed in Hs 695 T cells.
-
Chem Asian J
Selective Protein Degradation through Tetrazine Ligation of Genetically Incorporated Unnatural Amino Acids. [Abstract]2024 Sep 2:e202400824. PMID: 39221720 -
J Cancer
2025 Oct 1;16(14):4206-4218. PMID: 41210680 -
Cell Biol Int
Solute Carrier Family 19 Member 1 Mediates Acquired Bortezomib Resistance in Multiple Myeloma Through Chronic Stimulator of Interferon Genes Activation and Mitochondrial DNA Release. [Abstract]2026 Feb;50(2):e70130. PMID: 41556422 -
Front Biosci (Landmark Ed)
Cisplatin Disrupts Proteasome Bounce-Back Effect through Suppressing ZEB1/Nfe2l1 in Cholangiocarcinoma. [Abstract]2024 Mar 15;29(3):106. PMID: 38538281 -
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Inhibition of CARM1 suppresses proliferation of multiple myeloma cells through activation of p53 signaling pathway. [Abstract]2023 Sep;50(9):7457-7469. PMID: 37477799 -
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2021 Aug 5:12:678368. PMID: 34421991 -
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The ubiquitin-proteasome system is essential for efficient propagation of Pseudorabies virus. [Abstract]2025 Jun 13:307:110602. PMID: 40517584 -
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Chorioallantoic membrane (CAM) assay to study treatment effects in diffuse intrinsic pontine glioma. [Abstract]2022 Feb 14;17(2):e0263822. PMID: 35157705 -
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bioRxiv
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bioRxiv
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bioRxiv
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bioRxiv
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Oncotarget
LP-284, a small molecule acylfulvene, exerts potent antitumor activity in preclinical non-Hodgkin's lymphoma models and in cells deficient in DNA damage repair. [Abstract]2023 Jun 12:14:597-611. PMID: 37306526 -
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Lösungsmittel & Löslichkeit
Ethanol : 66.67 mg/mL (173.51 mM; ultrasonic and warming and heat to 60°C)
DMSO : 50 mg/mL (130.13 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (40.0 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (40.0 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.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 4 mg/mL (10.41 mM); Clear solution
This protocol yields a clear solution of ≥ 4 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 EtOH stock solution (40.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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)
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.
Reinheit & Dokumentation
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Data Sheet (283 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Adams J, et al. Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res. 1999 Jun 1;59(11):2615-22. [Content Brief]
[2]. Shahshahan MA, et al. Potential usage of proteasome inhibitor bortezomib (Velcade, PS-341) in the treatment of metastaticmelanoma: basic and clinical aspects. Am J Cancer Res. 2011;1(7):913-24. [Content Brief]
[3]. Pérez-Galán P, et al. The proteasome inhibitor bortezomib induces apoptosis in mantle-cell lymphoma through generation of ROS and Noxa activation independent of p53 status. Blood. 2006 Jan 1;107(1):257-64. [Content Brief]
[4]. Yerlikaya A, et al. Combined effects of the proteasome inhibitor bortezomib and Hsp70 inhibitors on the B16F10 melanoma cell line. Mol Med Rep. 2010 Mar-Apr;3(2):333-9. [Content Brief]
[5]. Mujtaba T, et al. Advances in the understanding of mechanisms and therapeutic use of bortezomib. Discov Med. 2011 Dec;12(67):471-80. [Content Brief]
[6]. Fernández Y, et al. Chemical blockage of the proteasome inhibitory function of bortezomib: impact on tumor cell death. J Biol Chem. 2006 Jan 13;281(2):1107-18. [Content Brief]
[7]. Wang Y, et al. TREM2-Mediated Cholesterol Efflux in Macrophages Inhibits Anti-Tumor Immunity via Limitation of CD4+ T and NK Cells. Adv Sci (Weinh). 2025 Oct 20:e06995. [Content Brief]
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). 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 / Ethanol | 1 mM | 2.6025 mL | 13.0127 mL | 26.0254 mL | 65.0635 mL |
| 5 mM | 0.5205 mL | 2.6025 mL | 5.2051 mL | 13.0127 mL | |
| 10 mM | 0.2603 mL | 1.3013 mL | 2.6025 mL | 6.5064 mL | |
| 15 mM | 0.1735 mL | 0.8675 mL | 1.7350 mL | 4.3376 mL | |
| 20 mM | 0.1301 mL | 0.6506 mL | 1.3013 mL | 3.2532 mL | |
| 25 mM | 0.1041 mL | 0.5205 mL | 1.0410 mL | 2.6025 mL | |
| 30 mM | 0.0868 mL | 0.4338 mL | 0.8675 mL | 2.1688 mL | |
| 40 mM | 0.0651 mL | 0.3253 mL | 0.6506 mL | 1.6266 mL | |
| 50 mM | 0.0521 mL | 0.2603 mL | 0.5205 mL | 1.3013 mL | |
| 60 mM | 0.0434 mL | 0.2169 mL | 0.4338 mL | 1.0844 mL | |
| 80 mM | 0.0325 mL | 0.1627 mL | 0.3253 mL | 0.8133 mL | |
| 100 mM | 0.0260 mL | 0.1301 mL | 0.2603 mL | 0.6506 mL |