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Home >> Signaling Pathways >> Ubiquitination/ Proteasome >> Proteasome

Proteasome

The proteasome is a large multisubunit complex of approximately 2.5 MDa that mediates a wide range of physiological and pathological cellular processes by selectively degrading unnecessary proteins in eukaryotes. The structure of a proteasome is comprised of the catalytic core particle (CP) and two terminal regulatory particles (RPs). The CP (also known as the 20S proteasome) is a barrel shaped multisubunit complex (approximately 750 kDa) consisting of four axially stacked heptameric rings (two outer α-rings and two inner β-rings) with 7 subunits in each ring, where three β subunits (β1, β2 and β5) contain catalytically active threonine residues and are associated with caspase-like, trypsin-like and chymotrypsin-like activities respectively.

Products for  Proteasome

  1. Cat.No. Product Name Information
  2. GC65547 (1S,2R)-Alicapistat (1S,2R)-Alicapistat ((1S,2R)-ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). (1S,2R)-Alicapistat Chemical Structure
  3. GC62193 (1S,2S)-Bortezomib (1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans. (1S,2S)-Bortezomib Chemical Structure
  4. GC41233 (R)-MG132

    A potent proteasome inhibitor

     (R)-MG132 Chemical Structure
  5. GC68503 20S Proteasome activator 1

    20S Proteasome activator 1 is an effective activator of the 20S protease, with IC50 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like sites, chymotrypsin-like sites and caspase-like sites respectively. It can be translated in cellular systems to prevent accumulation of pathogenic A53T mutant alpha-synuclein. 20S Proteasome activator 1 can be used for research on neurodegenerative diseases.

     20S Proteasome activator 1 Chemical Structure
  6. GC64472 20S Proteasome-IN-1 20S Proteasome-IN-1 is a 26S proteasome inhibitor extracted from patent WO2006128196A2 compound 2. 20S Proteasome-IN-1 Chemical Structure
  7. GC65668 5-Amino-8-hydroxyquinoline 5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity. 5-Amino-8-hydroxyquinoline Chemical Structure
  8. GC10102 Aclacinomycin A An anthracycline with antibiotic and anticancer activities Aclacinomycin A Chemical Structure
  9. GC35238 Aclacinomycin A hydrochloride Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors. Aclacinomycin A hydrochloride Chemical Structure
  10. GC33743 Alicapistat (ABT-957) Alicapistat (ABT-957) (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential application of Alzheimer's disease (AD). Alicapistat (ABT-957) Chemical Structure
  11. GC13789 AM 114 AM 114 Chemical Structure
  12. GC12784 Artemether (SM-224) An antiparasitic compound Artemether (SM-224) Chemical Structure
  13. GC17644 Bortezomib (PS-341) Bortezomib (PS-341), as a dipeptide boronic acid proteasome inhibitor with antitumor activity, can potently inhibiit 20S proteasome with Ki of 0.6 nM by targeting a threonine residue.. Bortezomib (PS-341) Chemical Structure
  14. GC65010 Bortezomib-d8 Bortezomib-d8 (PS-341-d8) is the deuterium labeled Bortezomib. 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. Anti-cancer activity. Bortezomib-d8 Chemical Structure
  15. GC12527 Calpain Inhibitor I, ALLN A non-selective cysteine protease inhibitor Calpain Inhibitor I, ALLN Chemical Structure
  16. GC40694 Calpain Inhibitor II Calpain Inhibitor II (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. Calpain Inhibitor II Chemical Structure
  17. GC67908 Calpain-2-IN-1 Calpain-2-IN-1 Chemical Structure
  18. GC10342 Calpeptin A calpain inhibitor Calpeptin Chemical Structure
  19. GC32815 Capzimin Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor. Capzimin Chemical Structure
  20. GC15089 Carfilzomib (PR-171) A proteasome inhibitor Carfilzomib (PR-171) Chemical Structure
  21. GC15083 Celastrol A triterpenoid antioxidant Celastrol Chemical Structure
  22. GC12272 CEP-18770 An inhibitor of chymotrypsin-like proteasome activity CEP-18770 Chemical Structure
  23. GC16581 Clasto-Lactacystin β-lactone A selective inhibitor of the 20S proteasome Clasto-Lactacystin β-lactone Chemical Structure
  24. GC64607 Dazcapistat Dazcapistat is a potent calpain inhibitor, with IC50s of <3 μM for calpain 1, calpain 2 and calpain 9, respectively (patent WO2018064119A1, compound 405). Dazcapistat Chemical Structure
  25. GC16747 Dihydroeponemycin Dihydroeponemycin Chemical Structure
  26. GC12494 Epoxomicin A highly selective proteasome inhibitor Epoxomicin Chemical Structure
  27. GC31563 FK-448 Free base FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM. FK-448 Free base Chemical Structure
  28. GC13711 Gabexate mesylate A serine protease inhibitor Gabexate mesylate Chemical Structure
  29. GC17255 Gliotoxin An immunosuppressive mycotoxin with diverse biological effects Gliotoxin Chemical Structure
  30. GC64213 GSK3494245 GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. GSK3494245 Chemical Structure
  31. GC16699 HMB-Val-Ser-Leu-VE inhibitor of the trypsin-like activity of the 20S proteasome HMB-Val-Ser-Leu-VE Chemical Structure
  32. GC36356 Ixazomib citrate Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM. Ixazomib citrate Chemical Structure
  33. GC31899 KZR-504 KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 Chemical Structure
  34. GC13123 Lactacystin (Synthetic)

    A selective inhibitor of the 20S proteasome

     Lactacystin (Synthetic) Chemical Structure
  35. GC34649 LMP7-IN-1 LMP7-IN-1 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. LMP7-IN-1 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. LMP7-IN-1 shows strong antitumor efficacy in multiple myeloma xenograft models. LMP7-IN-1 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells. LMP7-IN-1 Chemical Structure
  36. GC64282 LXE408 LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 Chemical Structure
  37. GC11640 MDL 28170 A cell permeable, selective calpain inhibitor MDL 28170 Chemical Structure
  38. GC10178 MG-115 A potent, reversible proteasome inhibitor MG-115 Chemical Structure
  39. GC10383 MG-132

    A potent proteasome inhibitor

     MG-132 Chemical Structure
  40. GC15517 MG-262 A proteasome inhibitor with diverse biological activities MG-262 Chemical Structure
  41. GC16146 MLN2238 A 20S proteasome inhibitor and an active metabolite of MLN9708 MLN2238 Chemical Structure
  42. GC13718 MLN9708 A prodrug form of MLN2238 MLN9708 Chemical Structure
  43. GC15778 ONX-0914 (PR-957) A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome ONX-0914 (PR-957) Chemical Structure
  44. GC62210 ONX-0914 TFA ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA Chemical Structure
  45. GC15447 Oprozomib (ONX-0912) An orally available proteasome inhibitor Oprozomib (ONX-0912) Chemical Structure
  46. GC16912 PD 150606 An inhibitor of calpains PD 150606 Chemical Structure
  47. GC10561 PD 151746 calpain inhibitor, cell-permeable PD 151746 Chemical Structure
  48. GC11974 Pepstatin A

    Pepstatin A is an orally active inhibitor of aspartic proteases, which is produced by actinomycetes.

     Pepstatin A Chemical Structure
  49. GC36871 Pepstatin Ammonium Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium Chemical Structure
  50. GC36872 Pepstatin Trifluoroacetate Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Trifluoroacetate Chemical Structure
  51. GC15802 PI-1840 Chymotrypsin-like (CT-L) inhibitor PI-1840 Chemical Structure
  52. GC63964 PR-39 TFA PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFA Chemical Structure
  53. GC61945 PR-924 PR-924 is a selective tripeptide epoxyketone immunoproteasome subunit LMP-7 inhibitor with an IC50 of 22 nM. PR-924 covalently modifies proteasomal N-terminal threonine active sites. PR-924 inhibits growth and triggers apoptosis in multiple myeloma (MM) cells. PR-924 has antitumor activities. PR-924 Chemical Structure
  54. GC33311 Proteasome-IN-1 Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. Proteasome-IN-1 Chemical Structure
  55. GC13865 PSI PSI Chemical Structure
  56. GC61221 PTP1B-IN-9 PTP1B-IN-9 is a ubiquitin-proteasome system (UPS)-stressor. PTP1B-IN-9 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. PTP1B-IN-9 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity. PTP1B-IN-9 Chemical Structure
  57. GC32765 RA190 RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. RA190 Chemical Structure
  58. GC62399 RA375 RA375 is a RPN13 (26S proteasome regulatory subunit) inhibitor. RA375 activates UPR signaling, ROS production and apoptosis. RA375 exhibits ten-fold greater activity against cancer lines than RA190, reflecting its nitro ring substituents and the addition of a chloroacetamide warhead. RA375 Chemical Structure
  59. GC32407 Rpn11-IN-1 Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM. Rpn11-IN-1 Chemical Structure
  60. GC10486 Salinosporamide A (NPI-0052, Marizomib) An orally bioactive proteasome inhibitor Salinosporamide A (NPI-0052, Marizomib) Chemical Structure
  61. GC39166 TCH-165 TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation. TCH-165 Chemical Structure
  62. GC65938 Thrombin inhibitor 5 Thrombin inhibitor 5 (compound 385) is a thrombin inhibitor, with IC50s ranging from 0.1 μM to 1 μM. Thrombin inhibitor 5 can be used for research of venous thromboembolism. Thrombin inhibitor 5 Chemical Structure
  63. GC37814 Tomatine Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill. Tomatine Chemical Structure
  64. GC68437 Vimentin-IN-1 Vimentin-IN-1 Chemical Structure
  65. GC12003 VR23 proteasome inhibitor VR23 Chemical Structure
  66. GA23841 Z-Ile-Glu(OtBu)-Ala-Leu-aldehyde Z-IE(OtBu)AL-CHO is an inhibitor of chymotrypsin-like activity of the multicatalytic proteinase complex (MPC; 20S proteasome) in HT4 cells. It is the first inhibitor reported so far which can cause accumulation of ubiquitinylated proteins in neuronal cells. Furthermore, this compound induced massive apoptosis in murine leukaemia L1210 cells. Therefore, proteasome inhibitors may be considered as potential anti-neoplastic agents. Z-Ile-Glu(OtBu)-Ala-Leu-aldehyde Chemical Structure
  67. GC62239 Zetomipzomib Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib Chemical Structure

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