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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)-ABT-957

     (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

    (R)-MG132 is a proteasome inhibitor with an IC50 of 100 nM.

     (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

    5A8HQ

     5-Amino-8-hydroxyquinoline (5A8HQ), a potential anticancer candidate, has promising proteasome inhibitory activity. 5-Amino-8-hydroxyquinoline Chemical Structure
  8. GC10102 Aclacinomycin A

    NSC 208734

     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)

    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

    PS-IX; AM114

     AM 114 Chemical Structure
  12. GC73863 ARI-3144 ARI-3144 is an excellent substrate for fibroblast activation protein (FAP). ARI-3144 Chemical Structure
  13. GC12784 Artemether (SM-224)

    (+)-Artemether, SM-224

     An antiparasitic compound Artemether (SM-224) Chemical Structure
  14. GC72901 BC-23

    NSC 45382

     BC-23 (NSC 45382) is a proteasome inhibitor. BC-23 Chemical Structure
  15. GC17644 Bortezomib (PS-341)

    LDP-341, MG-341, MLN341, NSC 681239, 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
  16. GC65010 Bortezomib-d8

    PS-341-d8; LDP-341-d8; NSC 681239-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
  17. GC40694 Calpain Inhibitor II

    AcLeuLeuMetH, ALLM

     Calpain Inhibitor II (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. Calpain Inhibitor II Chemical Structure
  18. GC67908 Calpain-2-IN-1 Calpain-2-IN-1 Chemical Structure
  19. GC10342 Calpeptin Calpeptin is a reversible and cell-permeable cysteine cathepsin inhibitor. The ID50 values of Calpeptin for calpain I and II (porcine), papain, and platelet calpain I are 52nM, 34nM, 138nM, and 20nM, respectively. Calpeptin alleviates apoptosis and secondary inflammatory changes in muscle cells. Calpeptin Chemical Structure
  20. GC32815 Capzimin Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor. Capzimin Chemical Structure
  21. GC15089 Carfilzomib (PR-171)

    PR-171

     A proteasome inhibitor Carfilzomib (PR-171) Chemical Structure
  22. GC15083 Celastrol Celastrol is a proteasome inhibitor with a potent and preferred inhibition of purified 20S proteasome with an IC50 of 2.5 μM. Celastrol Chemical Structure
  23. GC92062 CellFluor™ GST

    Cell Fluor™ Glutathione S-Transferase; DNs-Rh; bis-DNs-Rh

     CellFluor GST is a cell-permeable quenched fluorescent probe for the detection of pan-glutathione S-transferase activity in adherent or suspension cells, cell or tissue lysates, or purified enzyme preparations. CellFluor™ GST Chemical Structure
  24. GC12272 CEP-18770

    CEP-18770

     An inhibitor of chymotrypsin-like proteasome activity CEP-18770 Chemical Structure
  25. GC16581 Clasto-Lactacystin β-lactone

    β-Clastolactacystin; Omuralide

     A selective inhibitor of the 20S proteasome Clasto-Lactacystin β-lactone Chemical Structure
  26. 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
  27. GC72910 DD1 DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 Chemical Structure
  28. GC16747 Dihydroeponemycin

    Dihydroeponemycin,uk101

     Dihydroeponemycin Chemical Structure
  29. GC12494 Epoxomicin

    BU 4061T

     Epoxomicin is a selective proteasome inhibitor that effectively inhibits the chymotrypsin-like (CH-L) activity of the 20S proteasome, with an IC50 of approximately 40-80nM. Epoxomicin Chemical Structure
  30. GC70568 FiVe1 FiVe1 is a potent vimentin (VIM; the intermediate filament and mesenchymal marker) inhibitor. FiVe1 Chemical Structure
  31. 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
  32. GC13711 Gabexate mesylate A serine protease inhibitor Gabexate mesylate Chemical Structure
  33. GC17255 Gliotoxin

    Aspergillin

     Gliotoxin, an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi, is a specific inhibitor of 20S proteasomal chymotrypsin activity with an IC50 of 10μM. Gliotoxin Chemical Structure
  34. GC64213 GSK3494245

    DDD01305143?

     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
  35. GC16699 HMB-Val-Ser-Leu-VE inhibitor of the trypsin-like activity of the 20S proteasome HMB-Val-Ser-Leu-VE Chemical Structure
  36. 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
  37. 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
  38. GC13123 Lactacystin (Synthetic)

    A selective inhibitor of the 20S proteasome

     Lactacystin (Synthetic) Chemical Structure
  39. 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
  40. GC71416 LU-002i LU-002i is a subunit-selective human proteasome β2c and β2i inhibitor with an IC50 value of 220 nM for β2i. LU-002i Chemical Structure
  41. GC64282 LXE408 LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 Chemical Structure
  42. GC11640 MDL 28170

    MDL 28170

     MDL 28170, a cell permeable, reversible, peptidic aldehyde inhibitor of calpain (Ki= 0.01µM; Ki for cathepsin B = 0.025µM). MDL 28170 Chemical Structure
  43. GC12527 MG-101 (Calpain Inhibitor I, ALLN)

    AcLeuLeuNleAldehyde, ALLN, MG 101

     MG-101 (Calpain Inhibitor I, ALLN) also known as Calpain Inhibitor I, selectively inhibits various cysteine proteases, including calpain I, calpain II, cathepsin B, and cathepsin L. The corresponding Ki values for these enzymes are 90pM, 220pM, 150pM, and 500pM. MG-101 (Calpain Inhibitor I, ALLN) Chemical Structure
  44. GC10178 MG-115 MG-115 is a potent inhibitor with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 Chemical Structure
  45. GC10383 MG-132

    ZLeuLeuLeuCHO

     MG-132 is a potent, reversible, and cell-permeable proteasome inhibitor. MG-132 Chemical Structure
  46. GC15517 MG-262

    PS-III,MG262,MG 262

     A proteasome inhibitor with diverse biological activities MG-262 Chemical Structure
  47. GC16146 MLN2238 A 20S proteasome inhibitor and an active metabolite of MLN9708 MLN2238 Chemical Structure
  48. GC13718 MLN9708

    Ixazomib Citrate

     A prodrug form of MLN2238 MLN9708 Chemical Structure
  49. GC15778 ONX-0914 (PR-957)

    ONX-0914,PR-957

     ONX-0914 (PR-957) is a specific inhibitor of the immunoproteasome subunits low molecular weight polypeptide 7 (LMP7) and low molecular weight polypeptide 2 (LMP2), with IC50 values of 0.34μM and 0.0057μM, respectively. ONX-0914 (PR-957) Chemical Structure
  50. GC62210 ONX-0914 TFA

    PR-957 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
  51. GC15447 Oprozomib (ONX-0912)

    ONX-0912,ONX0912,ONX 0912,PR 047,Oprozomib

     An orally available proteasome inhibitor Oprozomib (ONX-0912) Chemical Structure
  52. GC16912 PD 150606 An inhibitor of calpains PD 150606 Chemical Structure
  53. GC10561 PD 151746 calpain inhibitor, cell-permeable PD 151746 Chemical Structure
  54. GC11974 Pepstatin A

    NSC 272671, Pepsin Inhibitor S 735A

     Pepstatin A is an orally active inhibitor of aspartic proteases, which is produced by actinomycetes. Pepstatin A Chemical Structure
  55. GC36871 Pepstatin Ammonium

    Pepstatin A 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
  56. 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
  57. GC15802 PI-1840 Chymotrypsin-like (CT-L) inhibitor PI-1840 Chemical Structure
  58. 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
  59. 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
  60. GC33311 Proteasome-IN-1 Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. Proteasome-IN-1 Chemical Structure
  61. GC13865 PSI PSI Chemical Structure
  62. GC61221 PTP1B-IN-9

    NSC 638643

     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
  63. GC32765 RA190 RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13. RA190 Chemical Structure
  64. 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
  65. GC32407 Rpn11-IN-1

    Capzimin intermediate

     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
  66. GC10486 Salinosporamide A (NPI-0052, Marizomib)

    Marizomib, ML-858, NPI-0052

     Salinosporamide A (NPI-0052, Marizomib) is a 20S proteasome inhibitor isolated from the obligate marine actinobacterium Salinispora tropica, exhibiting potent antitumor activity with an IC50 value of 1.3nM. Salinosporamide A (NPI-0052, Marizomib) Chemical Structure
  67. 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
  68. 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
  69. GC37814 Tomatine Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill. Tomatine Chemical Structure
  70. GC68437 Vimentin-IN-1 Vimentin-IN-1 Chemical Structure
  71. GC12003 VR23 proteasome inhibitor VR23 Chemical Structure
  72. GC91968 WYneC

    Wittig-alkyne C

     WYneC is a chemoselective probe for the detection of sulfenylated proteins in live cells. WYneC Chemical Structure
  73. GC92015 WYneN

    Wittig-alkyne N

     WYneN is a chemoselective probe for the detection of sulfenylated proteins in live cells. WYneN Chemical Structure
  74. GC92016 WYneO

    Wittig-alkyne O

     WyneO is a probe for the detection of sulfenylated proteins. WYneO Chemical Structure
  75. GC62239 Zetomipzomib

    KZR-616

     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
  76. GC70395 Zetomipzomib maleate Zetomipzomib (KZR-616) maleate, a first-in-class immunoproteasome inhibitor, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP2/mLMP2) subunits of the immunoproteasome. Zetomipzomib maleate Chemical Structure

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