Proteasome

The proteasome complex is a broad spectrum protease present in all eukaryotes, which functions to carry out selective, efficient and progressive hydrolysis of intracellular target proteins. The proteasome plays a prominent role in the control of a diverse array of basic cellular processes.

Products
Background
Literature (2)
Gene Data

Proteasome Modulators

Cat. No. Product Name / Activity
7489 TCH-165
Enhancer of 20S proteasome assembly and 20S-mediated protein degradation

Proteasome Inhibitors

Cat. No. Product Name / Activity
7282 Bortezomib
High affinity proteasome inhibitor
6781 Capzimin dimer
Selective proteasome inhibitor
7188 Carfilzomib
Potent irreversible proteasome inhibitor; active in vivo
2267 Lactacystin
Cell-permeable, potent and selective proteasome inhibitor
1748 MG 132
Proteasome and calpain inhibitor. Inhibits NF-κB activation
6033 (R)-MG 132
Potent 20S proteasome inhibitor

The proteasome complex is a broad spectrum protease present in all eukaryotes, which functions to carry out selective, efficient and progressive hydrolysis of intracellular target proteins. The proteasome plays a prominent role in the control of a diverse array of basic cellular processes by rapidly catalyzing numerous biological reactions.

The proteasome complex is composed of a 20S catalytic core and one or two terminal 19S regulatory units. The 20S catalytic domain is barrel-shaped and consists of seven structurally similar α- and β-subunits. In the inactive state, the external α-subunits act as a physical barrier to prevent peptide substrates accessing the active site on the β-subunits. The 19S regulatory units recognize proteins marked by polyubiquitin chains, remove the chain, entrap the protein moiety and open the 20S α-subunits allowing the β-subunits to degrade the protein. Assembly of the 20S domain is very complex and requires extrinsic (e.g. PAC1) and intrinsic (e.g. C-tail of β-subunits) chaperones. The assembly mechanism of the 19S domain is poorly understood, but Hsp90 is thought to play a role.

Regulation of the proteasome complex is mediated by proteasome interacting proteins (PIPs). There are two classes of PIPs; protein factors related to the ubiquitylation system such as the deubiquitinating enzyme, USP14, and auxillary factors that regulate proteasome functions via direct binding, for example Ecm29.

External sources of pharmacological information for Proteasome :

    Literature for Proteasome

    Tocris offers the following scientific literature for Proteasome to showcase our products. We invite you to request* your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


    TPD and Induced Proximity Research Product Guide

    TPD and Induced Proximity Research Product Guide

    This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

    • Active Degraders
    • TAG Degradation Platform
    • Degrader Building Blocks
    • Assays for Protein Degradation
    • Induced Proximity Tools
    Targeted Protein Degradation Poster

    Targeted Protein Degradation Poster

    Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia

    Proteasome Gene Data

    Gene Species Gene Symbol Gene Accession No. Protein Accession No.
    α1 Human PSMA1 NM_002786 P25786
    Mouse Psma1 NM_011965 Q9R1P4
    Rat Psma1 NM_017278 P18420
    α2 Human PSMA2 NM_002787 P25787
    Mouse Psma2 NM_008944 P49722
    Rat Psma2 NM_017279 Q6P9V5
    α3 Human PSMA3 NM_002788 P25788
    Mouse Psma3 NM_011184 O70435
    Rat Psma3 NM_017280 P18422
    α4 Human PSMA4 NM_002789 P25789
    Mouse Psma4 NM_011966 Q9R1P0
    Rat Psma4 NM_017281 P21670
    α5 Human PSMA5 NM_002790 P28066
    Mouse Psma5 NM_011967 Q9Z2U1
    Rat Psma5 NM_017282 P34064
    α6 Human PSMA6 NM_002791 P60900
    Mouse Psma6 NM_011968 Q9QUM9
    Rat Psma6 NM_017283 P60901
    α7 Human PSMA7 NM_002792 O14818
    Mouse Psma7 NM_011969 Q9Z2U0
    Rat Psma7 NM_001008217 P48004
    α8 Human PSMA8 NM_144662 Q8TAA3
    Mouse Psma8 AK010717 Q9CWH6
    β1 Human PSMB1 NM_002793 P20618
    Mouse Psmb1 NM_011185 O09061
    Rat Psmb1 NM_053590 P18421
    β2 Human PSMB2 NM_002794 P49721
    Mouse Psmb2 NM_011970 Q9R1P3
    Rat Psmb2 NM_017284 P40307
    β3 Human PSMB3 NM_002795 P49720
    Mouse Psmb3 NM_011971 Q9R1P1
    Rat Psmb3 NM_017285 P40112
    β4 Human PSMB4 NM_002796 P28070
    Mouse Psmb4 NM_008945 P99026
    Rat Psmb4 NM_031629 P34067
    β5 Human PSMB5 NM_002797 P28074
    Mouse Psmb5 NM_011186 O55234
    Rat Psmb5 NM_001105727 P28075
    β6 Human PSMB6 NM_002798 P28072
    Mouse Psmb6 NM_008946 Q60692
    Rat Psmb6 NM_057099 P28073
    β7 Human PSMB7 NM_002799 Q99436
    Mouse Psmb7 NM_011187 P70195
    Rat Psmb7 NM_053532 Q9JHW0
    β8 Human PSMB8 NM_004159 P28062
    Mouse Psmb8 NM_010724 P28063
    Rat Psmb8 NM_080767 P28064
    β9 Human PSMB9 NM_148954 P28065
    Mouse Psmb9 NM_013585 P28076
    Rat Psmb9 NM_012708 P28077
    β10 Human PSMB10 NM_002801 P40306
    Mouse Psmb10 NM_013640 O35955
    Rat Psmb10 NM_001025637 Q4KM35
    β11 Human PSMB11 NM_001099780 A5LHX3
    Mouse Psmb11 NM_175204 Q8BG41
    Rat Psmb11 NM_001106032 XP_224175
    ATPase 1 Human PSMC1 NM_002802 P62191
    Mouse Psmc1 NM_008947 P62192
    Rat Psmc1 NM_057123 P62193
    ATPase 2 Human PSMC2 NM_002803 P35998
    Mouse Psmc2 NM_011188 P46471
    Rat Psmc2 NM_033236 Q63347
    ATPase 3 Human PSMC3 NM_002804 P17980
    Mouse Psmc3 NM_008948 O88685
    Rat Psmc3 NM_031595 Q63569
    ATPase 4 Human PSMC4 NM_006503 P43686
    Mouse Psmc4 NM_011874 P54775
    Rat Psmc4 NM_057122 Q63570
    ATPase 5 Human PSMC5 NM_002805 P62195
    Mouse Psmc5 NM_008950 P62196
    Rat Psmc5 NM_031149 O35050
    ATPase 6 Human PSMC6 NM_002806 P62333
    Mouse Psmc6 NM_025959 P62334
    Rat Psmc6 NM_001100509 Q32PW9
    Non-ATPase 1 Human PSMD1 NM_002807 Q99460
    Mouse Psmd1 NM_027357 Q3TXS7
    Rat Psmd1 NM_031978 O88761
    Non-ATPase 2 Human PSMD2 NM_002808 Q13200
    Mouse Psmd2 NM_134101 Q8VDM4
    Rat Psmd2 NM_001031639 Q4FZT9
    Non-ATPase 3 Human PSMD3 NM_002809 O43242
    Mouse Psmd3 NM_009439 P14685
    Rat Psmd3 NM_001008281 Q5U2S7
    Non-ATPase 4 Human PSMD4 NM_002810 P55036
    Mouse Psmd4 NM_008951 O35226
    Rat Psmd4 NM_031331 O88321
    Non-ATPase 5 Human PSMD5 NM_005047 Q16401
    Mouse Psmd5 NM_080554 Q8BJY1
    Rat Psmd5 NM_001106569 XP_216041
    Non-ATPase 6 Human PSMD6 NM_014814 Q15008
    Mouse Psmd6 NM_025550 Q99JI4
    Rat Psmd6 NM_198730 Q6PCT9
    Non-ATPase 7 Human PSMD7 NM_002811 P51665
    Mouse Psmd7 NM_010817 P26516
    Rat Psmd7 NM_001107426 XP_226439
    Non-ATPase 8 Human PSMD8 NM_002812 P48556
    Mouse Psmd8 NM_026545 Q9CX56
    Rat Psmd8 NM_001100831 Q3B8P5
    Non-ATPase 9 Human PSMD9 NM_002813 O00233
    Mouse Psmd9 NM_026000 Q9CR00
    Rat Psmd9 NM_130430 Q9WTV5
    Non-ATPase 10 Human PSMD10 NM_170750 O75832
    Mouse Psmd10 NM_016883 Q9Z2X2
    Rat Psmd10 NM_053925 Q9Z2X3
    Non-ATPase 11 Human PSMD11 NM_002815 O00231
    Mouse Psmd11 NM_178616 Q8BG32
    Rat Psmd11 NM_001107027 XP_220754
    Non-ATPase 12 Human PSMD12 NM_002816 O00232
    Mouse Psmd12 NM_025894 Q9D8W5
    Rat Psmd12 NM_001005875 Q5XIC6
    Non-ATPase 13 Human PSMD13 NM_002817 Q9UNM6
    Mouse Psmd13 NM_011875 Q9WVJ2
    Rat Psmd13 NM_001108925 XP_344977
    Non-ATPase 14 Human PSMD14 NM_005805 O00487
    Mouse Psmd14 NM_021526 O35593
    Rat Psmd14 NM_001025689 Q4V8E2