Ubiquitin/Proteasome

The ubiquitin-proteasome system (UPS) is a major intracellular protein degradation system in eukaryotes. Damaged, misfolded, or superfluous proteins are labeled with multiple ubiquitin molecules (a 76 amino acid peptide) via the sequential action of E1 activating enzyme, E2 conjugating enzyme, and E3 ligase ultimately leading to destruction of the protein by the 26S proteasome. Deubiquitinases cleave the bond between ubiquitin and protein. Dysregulation of the UPS and/or DUBs is implicated in many neurological disorders, cancer, atherosclerosis and other pathological states.

DUBS

  • MS102 | USP2 inhibitor
    CAS:
    N/A
    Catalog Number:
    10-4937
  • AZ1 | USP25/28 inhibitor
    CAS:
    2165322-94-9
    Catalog Number:
    10-4317
  • OTUDin3 | OTUD3 inhibitor
    CAS:
    441290-65-9
    Catalog Number:
    10-4981
  • iBAP-II | BAP1 inhibitor
    CAS:
    1013813-81-4
    Catalog Number:
    10-4038
    Activity:
    BAP1 inhibitor
    Chemical Names:
    4-(8-Nitro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-yl)phenol
    Molecular Weight:
    308.33
    Molecular Formula:
    C18H16N2O3
    Solubility:
    Soluble in DMSO (25 mg/ml)
    Physical Properties:
    Yellow solid
    Purity:
    >98% HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • P22077 | Selective USP7 inhibitor
    CAS:
    1247819-59-5
    Catalog Number:
    10-4125
    Activity:
    Selective USP7 inhibitor
    Chemical Name:
    1-(5-((2,4-Difluorophenyl)thio)-4-nitrothiophen-2-yl)ethanone
    Molecular Weight:
    315.32
    Molecular Formula:
    C12H7F2NO3S2
    Solubility:
    Soluble in DMSO (up to 25 mg/ml)
    Physical Properties:
    Off-white solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT

E3 Ubiquitin ligase

Other ligases

Other Ubiquitin/Proteasome

PROTACS

Proteasome

  • Ixazomib | Proteasome inhibitor
    CAS:
    1072833-77-2
    Catalog Number:
    10-5185
  • ONX-0914 | Immunoproteasome inhibitor
    CAS:
    960374-59-8
    Catalog Number:
    10-5885
  • Bortezomib | Proteasome inhibitor
    CAS:
    179324-69-7
    Catalog Number:
    10-2120
    Activity:
    Proteasome inhibitor
    Alternate Names:
    MG-341, PS-341
    Chemical Name:
    N-(2-Pyrazine)carbonyl-L-phenylalanine-L-leucine boronic acid
    Molecular Weight:
    384.25
    Molecular Formula:
    C19H25BN4O4
    Solubility:
    Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 35 mg/ml).
    Physical Properties:
    White solid
    Purity:
    98% by TLC
    NMR (conforms)
    Storage Temperature:
    -20°
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
    Shipping Code:
    RT
  • MG-132 | Proteasome inhibitor
    CAS:
    133407-82-6
    Catalog Number:
    10-1309
    Activity:
    Proteasome inhibitor
    Alternate Names:
    Z-Leu-Leu-Leu-CHO
    Chemical Name:
    N-(Benzyloxycarbonyl)leucinylleucinylleucinal
    Molecular Weight:
    475.63
    Molecular Formula:
    C26H41N3O5
    Solubility:
    Soluble in DMSO (up to 45 mg/ml), in DMF (up to 45 mg/ml), or in Ethanol (up to 45 mg/ml).
    Physical Properties:
    White solid
    Purity:
    98% by HPLC
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO, DMF or ethanol may be stored at -20° for up to 1 week.
    Shipping Code:
    RT
  • Z-Leu-Leu-Leu-vinylsulfone | Proteasome inhibitor
    CAS:
    193482-47-2
    Catalog Number:
    10-4990

Ubiquitin activating enzyme

  • ML-792 | SUMO-activating enzyme inhibitor
    CAS:
    1644342-14-2
    Catalog Number:
    10-4985
  • Pyr41 | E1 UAE inhibitor
    CAS:
    418805-02-4
    Catalog Number:
    10-1304
    Activity:
    E1 UAE inhibitor
    Chemical Name:
    4-[4-(5-Nitro-furan-2-ylmethylene)-3,5-dioxo-pyrazolidin-1-yl]-benzoic acid ethyl ester
    Molecular Weight:
    371.31
    Molecular Formula:
    C17H13N3O7
    Solubility:
    Soluble in DMSO (up to 25 mg/ml).
    Physical Properties:
    Brown solid
    Purity:
    98% by TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C (des.)
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 week.
    Shipping Code:
    RT

Ubiquitin-like modifiers

  • NAcM-OPT | NEDD8 ligation inhibitor
    CAS:
    2089293-61-6
    Catalog Number:
    10-1636
    Activity:
    NEDD8 ligation inhibitor
    Chemical Name:
    1-Benzyl-1-(1-butylpiperidin-4-yl)-3-(3,4-dichlorophenyl)urea
    Molecular Weight:
    434.40
    Molecular Formula:
    C23H29Cl2N3O
    Solubility:
    Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 20 mg/ml)
    Physical Properties:
    White solid
    Purity:
    98% by HPLC/TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year as from date of purchase supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • MLN4924 | NEDD8 activating enzyme inhibitor
    CAS:
    905579-51-3
    Catalog Number:
    10-1311
    Activity:
    NEDD8 activating enzyme inhibitor
    Chemical Name:
    ((1S,2S,4R)-4-(4-(((S)-2,3-Dihydro-1H-inden-1-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate; Pevonedistat
    Molecular Weight:
    443.53
    Molecular Formula:
    C21H25N5O4S
    Solubility:
    Soluble in DMSO (up to 10 mg/ml).
    Physical Properties:
    White solid
    Purity:
    98% by TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C (des.)
    Stability:
    Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
    Shipping Code:
    RT