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

  • 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
  • ML323 | USP-1/UAF-1 inhibitor
    CAS:
    1572414-83-5
    Catalog Number:
    10-1560
    Activity:
    USP-1/UAF-1 inhibitor
    Chemical Name:
    N-(4-(1H-1,2,3-Triazol-1-yl(benzyl)-5-methyl-2-(2-isopropylphenyl)pyrimidin-4-amine
    Alternate Names:
    CID 60167849; NCGC00262306
    Molecular Weight:
    384.48
    Molecular Formula:
    C23H24N6
    Solubility:
    Soluble in DMSO (up to 40 mg/ml), or in Ethanol (up to 20 mg/ml)
    Physical Properties:
    White solid
    Purity:
    98% by TLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
    Shipping Code:
    RT
  • TCID | DUB inhibitor
    CAS:
    30675-13-9
    Catalog Number:
    10-2428
    Activity:
    DUB inhibitor
    Chemical Name:
    4,5,6,7-Tetrachloro-1H-indene-1,3(2H)-dione
    Molecular Weight:
    283.93
    Molecular Formula:
    C9H2Cl4O2
    Solubility:
    Soluble in DMSO (up to 25 mg/ml),
    Physical Properties:
    White solid
    Purity:
    97% by TLC
    NMR (Conforms)
    Storage Temperature:
    RT
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
    Shipping Code:
    RT

E3 Ubiquitin ligase

  • SKPin C1 | Ubiquitin ligase E3 SCF-Skp2 inhibitor
    CAS:
    432001-69-9
    Catalog Number:
    10-1441
    Activity:
    Ubiquitin ligase E3 SCF-Skp2 inhibitor
    Chemical Names:
    2-[4-Bromo-2-[[4-oxo-3-(3-pyridinyl¬methyl)-2-thioxo-5-thiazolidinylidene]methyl]-phenoxy]acetic acid
    Molecular Weight:
    465.34
    Molecular Formula:
    C18H13BrN2O4S2
    Solubility:
    Soluble in DMSO (15 mg/ml with warming)
    Physical Properties:
    Yellow solid
    Purity:
    98% TLC
    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 2 month.
    Shipping Code:
    RT
  • Indisulam | RBM39 Molecular glue
    CAS:
    165668-41-7
    Catalog Number:
    10-3927
  • Iberdomide | Cereblon modulator/Molecular glue
    CAS:
    1323403-33-3
    Catalog Number:
    10-3921
  • CC-90009 | Cereblon modulator/Molecular glue
    CAS:
    1860875-51-9
    Catalog Number:
    10-3922
  • Adavosertib | Wee1 kinase inhibitor
    CAS:
    955365-80-7
    Catalog Number:
    10-4823
    Activity:
    Wee1 kinase inhibitor
    Chemical Names:
    1,2-Dihydro-1-[6-(1-hydroxy-1-methylethyl)-2-pyridinyl]-6-[[4-(4-methyl-1-piperazinyl)-phenyl]amino]-2-(2-propen-1-yl)-3H-pyrazolo[3,4-d]pyrimidin-3-one
    Alternate Name:
    MK-1775; AZD1775
    Molecular Weight:
    500.61
    Molecular Formula:
    C27H32N8O2
    Solubility:
    Soluble in DMSO (70 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

Other ligases

Other Ubiquitin/Proteasome

Proteasome

  • Z-Leu-Leu-Leu-vinylsulfone | Proteasome inhibitor
    CAS:
    193482-47-2
    Catalog Number:
    10-4990
  • Gliotoxin | Immunomodulator
    CAS:
    67-99-2
    Catalog Number:
    10-2076
    Activity:
    Immunomodulator
    Chemical Names:

    (3R,5aS,6S,10aR)-2,3,5a,6-Tetrahydro-6-hydroxy-3-(hydroxymethyl)-2-methyl-10H-3,10a-epidithiopyrazino
    [1,2-a]indole-1,4-dione; Aspergillin

    Molecular Weight:
    326.39
    Molecular Formula:
    C13H14N2O4S2
    Solubility:
    Soluble in DMSO (up to 15 mg/ml)
    Physical Properties:
    White lyophilized solid
    Purity:
    98%  HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°C
    Stability:
    Stable for 2 yeara as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • ML241 | p97 AAA ATPase inhibitor
    CAS:
    1346528-06-0
    Catalog Number:
    10-1555
    Activity:
    p97 AAA ATPase inhibitor
    Chemical Name:
    N-Benzyl-2-(2,3-dihydro-1,4-benzoxazin-4-yl)-5,6,7,8-tetrahydroquinazolin-4-amine
    Alternate Name:
    CID49830260
    Molecular Weight:
    372.46
    Molecular Formula:
    C23H24N4O
    Solubility:
    Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 14 mg/ml with warming).
    Physical Properties:
    Pale yellow solid
    Purity:
    98% by HPLC
    NMR (Conforms)
    Storage Temperature:
    -20°
    Stability:
    Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
    Shipping Code:
    RT
  • Suc-Leu-Leu-Val-Tyr-AMC | Proteasome substrate
    CAS:
    94367-21-2
    Catalog Number:
    10-2971
    Activity:
    Proteasome substrate
    Alternate Names:
    Suc-LLVY-AMC, Proteasome Substrate III (Fluorogenic)
    Molecular Weight:
    763.88
    Molecular Formula:
    C40H53N5O10
    Solubility:
    Soluble in DMSO (up to 20 mg/ml), or in DMF (up to 10 mg/ml)
    Physical Properties:
    Lyophilized 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 or DMF may be stored at -20°C for up to 1 month.
    Shipping Code:
    RT
  • Bz-Val-Gly-Arg-AMC | Proteasome substrate
    CAS:
    87779-49-5
    Catalog Number:
    10-2969
    Activity:
    Proteasome substrate
    Chemical Name:
    Benzoyl-Val-Gly-Arg-(7-amido-4-methylcoumarin)·trifluoroacetate
    Molecular Weight:
    705.7
    Molecular Formula:
    C30H37N7O6·CF3COOH
    Solubility:
    Soluble in DMSO.
    Physical Properties:
    White solid
    Purity:
    98% by HPLC
    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 month.
    Shipping Code:
    RT

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

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