1. Search Result
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Targets Recommended: E1/E2/E3 Enzyme
Results for "

ubiquitin

" in MCE Product Catalog:

208

Inhibitors & Agonists

1

Screening Libraries

2

Peptides

2

Natural
Products

35

Recombinant Proteins

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-100738
    Ubiquitin Isopeptidase Inhibitor I, G5

    NSC144303

    Apoptosis Cancer
    Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.
  • HY-103436
    NSC624206

    E1/E2/E3 Enzyme Cancer
    NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC50 of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC50=13 μM) but has no effect on ubiquitin adenylation.
  • HY-138698
    FT206

    Deubiquitinase Others
    FT206 is an inhibitor of carboxamides as ubiquitin-specific protrase extracted from patent WO 2020033707 A1, example 11-1.
  • HY-W054146
    RAMB4

    Proteasome Cancer
    RAMB4 is a ubiquitin-proteasome system (UPS)-stressor. RAMB4 inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activites. RAMB4 triggers a ubiquitin-proteasome-system (UPS)-stress response without affecting 20S proteasome catalytic activities. Anticancer activity.
  • HY-12989
    LDN-91946

    Deubiquitinase Cancer Neurological Disease
    LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a Ki app of 2.8 μM.
  • HY-122881
    HOIPIN-1

    JTP-0819958

    IKK Cancer
    HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro.
  • HY-44432
    Navitoclax-piperazine

    ABT-263-piperazine

    Bcl-2 Family Ligand for Target Protein for PROTAC Cancer
    Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor. Navitoclax-piperazine and a VHL ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC DT2216 (HY-130604).
  • HY-10949
    SMER3

    E1/E2/E3 Enzyme Cancer
    SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF) Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCF Met30.
  • HY-130683
    Lenalidomide-propargyl-C2-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-propargyl-C2-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Lenalidomide-propargyl-C2-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312).
  • HY-130682
    Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Lenalidomide-propargyl-C2-amido-Ph-NH2 hydrochloride can be used to design the PROTAC MD-224 (HY-114312).
  • HY-43722
    Lenalidomide-Br

    Ligand for E3 Ligase Cancer
    Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC STAT3 degrader SD-36 (HY-129602).
  • HY-N7695
    Physalin B

    Apoptosis Autophagy Cancer
    Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro.
  • HY-108468
    KL001

    Others Metabolic Disease
    KL001 is a first-in-class cryptochrome (CRY, a flavoproteins that are sensitive to blue light, and is involved in the circadian rhythms of plants and animals) stabilizer which specifically interacts with CRY1 and CRY2. KL001 prevents ubiquitin-dependent degradation of CRY, resulting in lengthening of the circadian period. KL001 has the potential to control fasting hormone-induced gluconeogenesis.
  • HY-108640
    HLI373

    MDM-2/p53 Parasite Apoptosis Cancer Infection
    HLI373 is an efficacious Hdm2 inhibitor. HLI373 inhibits the ubiquitin ligase activity of Hdm2. HLI373 is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
  • HY-108640A
    HLI373 dihydrochloride

    MDM-2/p53 Parasite Apoptosis Cancer Infection
    HLI373 dihydrochloride is an efficacious Hdm2 inhibitor. HLI373 dihydrochloride inhibits the ubiquitin ligase activity of Hdm2. HLI373 dihydrochloride is effective in inducing apoptosis of several tumor cells that are sensitive to DNA-damaging agents. Antimalarial activity.
  • HY-130815
    MAK683-CH2CH2COOH

    Histone Methyltransferase Ligand for Target Protein for PROTAC Cancer
    MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615).
  • HY-128756
    SIAIS178

    PROTACs Bcr-Abl Cancer
    SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC50 of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity.
  • HY-106443A
    Arimoclomol maleate

    BRX-220

    HSP Metabolic Disease Inflammation/Immunology Neurological Disease
    Arimoclomol maleate (BRX-220) is a co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
  • HY-123967
    RNF5 inhibitor inh-02

    Others Inflammation/Immunology
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
  • HY-133046
    VHL Ligand-Linker Conjugates 17

    E3 Ligase Ligand-Linker Conjugate Cancer
    VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.
  • HY-106443
    Arimoclomol

    BRX-220 free base

    HSP Metabolic Disease Inflammation/Immunology Neurological Disease
    Arimoclomol (BRX-220 free base) is a co-inducer of heat shock proteins (HSP). Arimoclomol protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
  • HY-106443B
    Arimoclomol citrate

    BRX-220 citrate

    HSP Metabolic Disease Inflammation/Immunology Neurological Disease
    Arimoclomol citrate (BRX-220 citrate) is a co-inducer of heat shock proteins (HSP). Arimoclomol citrate protects motor neurons by enhancing Hsp expression, thus directly affecting protein aggregation and clearance of misfolded assemblies via the proteasome-ubiquitin system.
  • HY-18638
    TCID

    4,5,6,7-Tetrachloroindan-1,3-dione

    Deubiquitinase Neurological Disease
    TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons.
  • HY-13453
    BAY 11-7082

    BAY 11-7821

    IKK Deubiquitinase Autophagy Apoptosis Cancer Inflammation/Immunology
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
  • HY-136242
    UT-34

    Androgen Receptor Cancer Endocrinology
    UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.
  • HY-100486
    BTTAA

    Others Others
    BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
  • HY-69220
    7-Octynoic acid

    PROTAC Linker Cancer
    7-Octynoic acid (compound 42) is a PROTAC linker and can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-120929
    BI8622

    E1/E2/E3 Enzyme Cancer
    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
  • HY-17540
    HBX 19818

    Deubiquitinase Cancer
    HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.
  • HY-120204
    BI8626

    E1/E2/E3 Enzyme Cancer
    BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM.
  • HY-100739
    RA190

    Proteasome Cancer
    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  • HY-50736
    DUB-IN-1

    Deubiquitinase Cancer
    DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
  • HY-100487
    TAK-243

    MLN7243

    E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
  • HY-112128
    USP7-IN-3

    Deubiquitinase Cancer
    USP7-IN-3 (Compound 5) is a potent and selective allosteric ubiquitin-specific protease 7 (USP7) inhibitor.
  • HY-129774
    Phthalimide-PEG4-MPDM-OH

    PROTAC Linker Cancer
    Phthalimide-PEG4-MPDM-OH is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-MPDM-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-130715
    tert-Butyl 11-aminoundecanoate

    PROTAC Linker Cancer
    tert-Butyl 11-aminoundecanoate (compound 6b) is a PROTAC linker, which refers to the PEG composition. tert-Butyl 11-aminoundecanoate can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-129773
    Phthalimide-PEG4-PDM-OTBS

    PROTAC Linker Cancer
    Phthalimide-PEG4-PDM-OTBS is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG4-PDM-OTBS can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-15667
    P005091

    P5091

    Deubiquitinase Cancer
    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
  • HY-13296
    PYR-41

    E1/E2/E3 Enzyme Apoptosis Cancer
    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
  • HY-16709
    USP7-IN-1

    Deubiquitinase Cancer
    USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
  • HY-18643
    TZ9

    E1/E2/E3 Enzyme Cancer
    TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.
  • HY-129772
    Phthalimide-PEG3-C2-OTs

    PROTAC Linker Cancer
    Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker, which refers to the PEGs composition. Phthalimide-PEG3-C2-OTs can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-40178
    NH2-C4-NH-Boc

    PROTAC Linker Cancer
    NH2-C4-NH-Boc (compound 15) is a PROTAC linker, which refers to the Alkyl/ether composition. NH2-C4-NH-Boc can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-12990
    Spautin-1

    Autophagy Apoptosis Cancer
    Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
  • HY-13865
    P 22077

    Deubiquitinase Cancer
    P 22077 is a cell-permeable ubiquitin-specific protease 7 (USP7) inhibitor with an EC50 of 8.01 μM. P 22077 also inhibits USP47 with an EC50 of 8.74 μM.
  • HY-111876
    SNIPER(TACC3)-1

    SNIPER Cancer
    SNIPER(TACC3)-1 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-1 induces cancer cell death.
  • HY-111877
    SNIPER(TACC3)-2

    SNIPER Cancer
    SNIPER(TACC3)-2 targets the TACC3 protein for degradation via the ubiquitin-proteasome pathway. SNIPER(TACC3)-2 induces cancer cell death.
  • HY-114304
    COH000

    E1/E2/E3 Enzyme Cancer
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
  • HY-125906
    VHL Ligand-Linker Conjugates 15

    E3 Ligase Ligand-Linker Conjugates 56

    E3 Ligase Ligand-Linker Conjugate Cancer
    VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs.
  • HY-A0003B
    Lenalidomide hemihydrate

    CC-5013 hemihydrate

    Ligand for E3 Ligase Molecular Glue Apoptosis Cancer
    Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-A0003
    Lenalidomide

    CC-5013

    Ligand for E3 Ligase Molecular Glue Apoptosis Cancer Inflammation/Immunology
    Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-A0003A
    Lenalidomide hydrochloride

    CC-5013 hydrochloride

    Ligand for E3 Ligase Molecular Glue Cancer Inflammation/Immunology
    Lenalidomide hydrochloride (CC-5013 hydrochloride), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hydrochloride is an orally active immunomodulator. Lenalidomide hydrochloride (CC-5013 hydrochloride) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hydrochloride (CC-5013 hydrochloride) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
  • HY-129395
    Mezigdomide

    CC-92480

    E1/E2/E3 Enzyme Molecular Glue Apoptosis Cancer
    Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating drug (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity.
  • HY-128822
    cIAP1 Ligand-Linker Conjugates 13

    E3 ligase Ligand-Linker Conjugates 43

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 13 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 13 can be used to design SNIPERs.
  • HY-128813A
    cIAP1 Ligand-Linker Conjugates 15 hydrochloride

    E3 ligase Ligand-Linker Conjugates 34 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 15 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 hydrochloride can be used to design SNIPERs.
  • HY-128815
    cIAP1 Ligand-Linker Conjugates 14

    E3 ligase Ligand-Linker Conjugates 36

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 14 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 14 can be used to design SNIPERs.
  • HY-128816A
    cIAP1 Ligand-Linker Conjugates 2 Hydrochloride

    E3 ligase Ligand-Linker Conjugates 37 Hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 2 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 Hydrochloride can be used to design SNIPERs.
  • HY-128820
    cIAP1 Ligand-Linker Conjugates 1

    E3 ligase Ligand-Linker Conjugates 41

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 1 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 1 can be used to design SNIPERs.
  • HY-128819
    cIAP1 Ligand-Linker Conjugates 3

    E3 ligase Ligand-Linker Conjugates 40

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 3 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 3 can be used to design SNIPERs.
  • HY-128826
    cIAP1 Ligand-Linker Conjugates 10

    E3 ligase Ligand-Linker Conjugates 47

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 10 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 10 can be used to design SNIPERs.
  • HY-128812A
    cIAP1 Ligand-Linker Conjugates 11 Hydrochloride

    E3 ligase Ligand-Linker Conjugates 33 Hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 11 Hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 Hydrochloride can be used to design SNIPERs.
  • HY-128813
    cIAP1 Ligand-Linker Conjugates 15

    E3 ligase Ligand-Linker Conjugates 34

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 15 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 can be used to design SNIPERs.
  • HY-128824
    cIAP1 Ligand-Linker Conjugates 9

    E3 ligase Ligand-Linker Conjugates 45

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 9 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 9 can be used to design SNIPERs.
  • HY-128812
    cIAP1 Ligand-Linker Conjugates 11

    E3 ligase Ligand-Linker Conjugates 33

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 11 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 can be used to design SNIPERs.
  • HY-128817
    cIAP1 Ligand-Linker Conjugates 12

    E3 ligase Ligand-Linker Conjugates 38

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 12 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 12 can be used to design SNIPERs.
  • HY-128825
    cIAP1 Ligand-Linker Conjugates 8

    E3 ligase Ligand-Linker Conjugates 46

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 8 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 8 can be used to design SNIPERs.
  • HY-128823
    cIAP1 Ligand-Linker Conjugates 7

    E3 ligase Ligand-Linker Conjugates 44

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 7 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 7 can be used to design SNIPERs.
  • HY-128818
    cIAP1 Ligand-Linker Conjugates 5

    E3 ligase Ligand-Linker Conjugates 39

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 5 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 5 can be used to design SNIPERs.
  • HY-128821
    cIAP1 Ligand-Linker Conjugates 4

    E3 ligase Ligand-Linker Conjugates 42

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 4 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 4 can be used to design SNIPERs.
  • HY-128816
    cIAP1 Ligand-Linker Conjugates 2

    E3 ligase Ligand-Linker Conjugates 37

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 2 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 can be used to design SNIPERs.
  • HY-128814
    cIAP1 Ligand-Linker Conjugates 6 hydrochloride

    E3 ligase Ligand-Linker Conjugates 35 hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    cIAP1 Ligand-Linker Conjugates 6 hydrochloride incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 6 hydrochloride can be used to design SNIPERs.
  • HY-130618
    Boc-C1-PEG3-C4-OH

    PROTAC Linker Cancer
    Boc-C1-PEG3-C4-OH is a PROTAC linker, which refers to the Alkyl/ether composition. Boc-C1-PEG3-C4-OH can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-123937
    THAL-SNS-032

    PROTACs CDK Cancer
    THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
  • HY-129168
    USP7-IN-5

    Deubiquitinase Cancer
    USP7-IN-5 is a potent ubiquitin specific protease 7 (USP7) inhibitor extracted from patent WO2017212012A1, example 40, has an IC50 of 49.9 nM.
  • HY-129169
    USP7-IN-6

    Deubiquitinase Cancer
    USP7-IN-6 is a potent ubiquitin specific protease 7 (USP7) inhibitor, extracted from patent WO2017212010A1, example 25, has an IC50 of 6.8 nM.
  • HY-111879
    Biotin-BS

    SNIPER Cancer
    Biotin-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and biotin, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
  • HY-111878
    BzNH-BS

    SNIPER Cancer
    BzNH-BS contains two different ligands, methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide, which are connected by linkers. MeBS as a ligand for cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase.
  • HY-N0170
    Indole-3-carbinol

    I3C; 3-Indolemethanol

    NF-κB Aryl Hydrocarbon Receptor E1/E2/E3 Enzyme Endogenous Metabolite Cancer
    Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
  • HY-15301
    CC0651

    E1/E2/E3 Enzyme Cancer
    CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27 Kip1, as confirmed by dose-response analysis.
  • HY-12025
    Serdemetan

    JNJ-26854165

    MDM-2/p53 E1/E2/E3 Enzyme Apoptosis Cancer
    Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
  • HY-124855
    STD1T

    Deubiquitinase Cancer
    STD1T is a deubiquitinase USP2a inhibitor with an IC50 of 3.3 μM in Ub-AMC Assay.
  • HY-16658B
    Z-VAD-FMK

    Z-VAD(OH)-FMK

    Caspase Cancer
    Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM.
  • HY-131232
    Desmorpholinyl Navitoclax-NH-Me

    Desmorpholinyl ABT-263-NH-Me

    Bcl-2 Family Ligand for Target Protein for PROTAC Cancer
    Desmorpholinyl Navitoclax-NH-Me is a Bcl-xL inhibitor. Desmorpholinyl Navitoclax-NH-Me and a CRBN ligand for the E3 ubiquitin ligase can be used in the synthesis of PROTAC BCL-XL degrader XZ739 (HY-133557).
  • HY-130619
    Boc-C1-PEG3-C4-OBn

    PROTAC Linker Cancer
    Boc-C1-PEG3-C4-OBn (PROTAC Linker 15) is a PROTAC linker, which refers to the PEG composition. Boc-C1-PEG3-C4-OBn can be used in the synthesis of a series of PROTACs, such as PROTAC SGK3 degrader-1 (HY-125878). PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.
  • HY-136163
    (S,R,S)-AHPC-C2-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-C2-NH2 dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-OH can be used in the synthesis of a series of PROTACs.
  • HY-128807
    E3 ligase Ligand 10

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-129653
    E3 ligase Ligand 18

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-128811
    E3 ligase Ligand 14

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-130270
    AhR Ligand-Linker Conjugates 1

    E3 Ligase Ligand-Linker Conjugates 57

    E3 Ligase Ligand-Linker Conjugate Cancer
    AhR Ligand-Linker Conjugates 1 (E3 Ligase Ligand-Linker Conjugates 57) incorporates an IAP ligand for the E3 ubiquitin ligase, and a SNIPER linker. AhR Ligand-Linker Conjugates 1 can be used to design SNIPER.
  • HY-43961
    E3 ligase Ligand 8

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-128810
    E3 ligase Ligand 13

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-13487
    USP7/USP47 inhibitor

    Deubiquitinase Cancer
    USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
  • HY-135844
    LS-102

    E1/E2/E3 Enzyme Inflammation/Immunology
    LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.
  • HY-128806
    E3 ligase Ligand 9

    Ligand for E3 Ligase Cancer
    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  • HY-133144
    Lenalidomide-OH

    Ligand for E3 Ligase Cancer
    Lenalidomide-OH is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-OH can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BTK degrader SJF620 (HY-133137).
  • HY-128842
    PROTAC MDM2 Degrader-3

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-128843
    PROTAC MDM2 Degrader-4

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-128840
    PROTAC MDM2 Degrader-1

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-1 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-1 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-128841
    PROTAC MDM2 Degrader-2

    PROTACs MDM-2/p53 E1/E2/E3 Enzyme Cancer
    PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-130988A
    Ipatasertib-NH2 dihydrochloride

    GDC-0068-NH2 dihydrochloride; RG7440-NH2 dihydrochloride

    Ligand for Target Protein for PROTAC Cancer
    Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-19726
    NSC59984

    MDM-2/p53 Cancer
    NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling.
  • HY-136160
    Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase, and a linker. Thalidomide 4'-oxyacetamide-alkyl-C2-amine hydrochloride can be used to design the PROTACs.
  • HY-130835
    FKBP12 PROTAC RC32

    RC32

    PROTACs FKBP Cancer
    FKBP12 PROTAC RC32 (RC32) is a potent FKBP12 degrader based on PROTAC technology. FKBP12 PROTAC RC32 contains conjugation of Rapamycin (HY-10219) and a ligand for an E3 ubiquitin ligase (Pomalidomide; HY-10984).
  • HY-131318
    Lenalidomide-I

    Ligand for E3 Ligase Cancer
    Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
  • HY-13297
    PYZD-4409

    E1/E2/E3 Enzyme Cancer
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
  • HY-111350
    FT827

    Deubiquitinase Cancer
    FT827 is a selective and covalent ubiquitin-specific protease 7 (USP7) inhibitor (Ki=4.2 µM). FT827 binds to the USP7 catalytic domain (USP7CD; residues 208-560) with an apparent Kd value of 7.8 µM.
  • HY-125292
    NV03

    Histone Methyltransferase Ligand for E3 Ligase Cancer
    NV03 is a potent and selective antagonist of UHRF1 (Ubiquitin-like with PHD and RING finger domains 1)- H3K9me3 interaction by binding to UHRF1 tandem tudor domain, with a Kd of 2.4 μM. NV03 has anticancer activity.
  • HY-108702
    ML-792

    E1/E2/E3 Enzyme Cancer
    ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50 values of 32 μM and >100 μM, respectively).
  • HY-122702
    PEG6-(CH2CO2H)2

    PROTAC Linker Others
    PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.
  • HY-111623
    USP30 inhibitor 11

    Deubiquitinase Cancer
    USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.
  • HY-130798
    (S,R,S)-AHPC-amido-C5-acid

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180).
  • HY-18637
    LDN-57444

    Deubiquitinase Apoptosis Neurological Disease
    LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
  • HY-19747
    HPOB

    HDAC Apoptosis Cancer
    HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6.
  • HY-112811
    PROTAC CDK9 degrader-2

    PROTACs CDK Cancer
    PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.
  • HY-110195
    Smurf1-IN-A01

    A01

    Others Others
    Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
  • HY-123872
    MSC1094308

    p97 Others
    MSC1094308 is a reversible and allosteric inhibitor of the type II AAA ATPase human ubiquitin-directed unfoldase (VCP)/p97 and the type I AAA ATPase VPS4B, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively.
  • HY-131189
    N-Boc-SBP-0636457-OH

    Ligand for E3 Ligase Cancer
    N-Boc-SBP-0636457-OH, a ligand for E3 ubiquitin ligase, is used in the recruitment of IAP E3 ligases. N-Boc-SBP-0636457-OH can be connected to the ligand for Bcl-xL by a linker to form PROTAC Bcl-xL degrader-1 (HY-131188).
  • HY-123844
    dBET57

    PROTACs Epigenetic Reader Domain Cancer
    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology. dBET57 mediates recruitment to the CRL4 CRBN E3 ubiquitin ligase, with a DC50/5h of 500 nM for BRD4BD1, and is inactive on BRD4BD2.
  • HY-130604
    DT2216

    PROTACs Apoptosis Cancer
    DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
  • HY-129241
    AGX51

    Others Cancer
    AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits pathologic ocular neovascularization.
  • HY-14658S
    Thalidomide D4

    Ligand for E3 Ligase Molecular Glue Autophagy Apoptosis Cancer Inflammation/Immunology
    Thalidomide D4 is a deuterium labeled Thalidomide. Thalidomide is initially promoted as a sedative, inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties.
  • HY-130713
    Thalidomide-C2-amido-C2-COOH

    E3 Ligase Ligand-Linker Conjugate Cancer
    Thalidomide-C2-amido-C2-COOH incorporates a CRBN ligand for the E3 ubiquitin ligase, and a linker. Thalidomide-C2-amido-C2-COOH can be used to design PROTAC CDK2/9 Degrader-1 (HY-130709).
  • HY-112937
    GNE-6640

    Deubiquitinase Cancer
    GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively.
  • HY-112098
    PROTAC ERα Degrader-1

    PROTACs Estrogen Receptor/ERR Cancer
    PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
  • HY-131385
    KB02-COOH

    Ligand for E3 Ligase Cancer
    KB02-COOH is a fragment of synthesis of ubiquitin E3 ligase ligand KB02. KB02 can be used in the synthesis of PROTAC, such as KB02-JQ1 (HY-129917) and KB02-SLF (HY-129610).
  • HY-117370
    USP25/28 inhibitor AZ1

    AZ1

    Deubiquitinase Cancer
    USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
  • HY-134817
    USP7-IN-8

    Deubiquitinase Cancer
    USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.
  • HY-103046
    UbcH5c-IN-1

    E1/E2/E3 Enzyme Inflammation/Immunology
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
  • HY-16658
    Z-VAD(OMe)-FMK

    Z-Val-Ala-Asp(OMe)-FMK

    Caspase Cancer
    Z-VAD(OMe)-FMK (Z-Val-Ala-Asp(OMe)-FMK) is a cell-permeable and irreversible pan-caspase inhibitor. Z-VAD(OMe)-FMK is an ubiquitin carboxy-terminal hydrolase L1 (UCHL1) inhibitor. Z-VAD(OMe)-FMK irreversibly modifies UCHL1 by targeting the active site of UCHL1.
  • HY-130988
    Ipatasertib-NH2

    GDC-0068-NH2; RG7440-NH2

    Ligand for Target Protein for PROTAC Cancer
    Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-136008A
    (S,R,S)-AHPC-PEG1-NH2 dihydrochloride

    VH032-PEG1-NH2 dihydrochloride

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-PEG1-NH2 dihydrochloride can be used to design PROTACs.
  • HY-17421
    Tenatoprazole

    TU-199

    Proton Pump Infection Inflammation/Immunology
    Tenatoprazole (TU-199) is an orally active imidazopyridine-based proton pump inhibitor with a prolonged plasma half-life. Tenatoprazole inhibits hog gastric H +/K +-ATPase activity with an IC50 of 6.2 μM. Tenatoprazole blocks the interaction of ubiquitin with the ESCRT-1 factor Tsg101, inhibits production of several enveloped viruses, including EBV.
  • HY-141178
    TCO-PEG3-amine

    PROTAC Linker Cancer
    TCO-PEG3-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141181
    TCO-PEG8-amine

    PROTAC Linker Cancer
    TCO-PEG8-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-133049
    Propargyl-PEG3-phosphonic acid

    PROTAC Linker Cancer
    Propargyl-PEG3-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130146
    Propargyl-PEG3-phosphonic acid diethyl ester

    PROTAC Linker Cancer
    Propargyl-PEG3-phosphonic acid diethyl ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130382
    Propargyl-PEG6-alcohol

    PROTAC Linker Cancer
    Propargyl-PEG6-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-121507
    Hydroxy-PEG2-C2-sulfonic acid

    PROTAC Linker Cancer
    Hydroxy-PEG2-C2-sulfonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130554
    m-PEG9-phosphonic acid

    PROTAC Linker Cancer
    m-PEG9-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141187
    TCO-PEG3-TCO

    PROTAC Linker Cancer
    TCO-PEG3-TCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-41921
    Propargyl-PEG3-alcohol

    PROTAC Linker Cancer
    Propargyl-PEG3-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130390
    Propargyl-PEG4-O-C1-NHS ester

    PROTAC Linker Cancer
    Propargyl-PEG4-O-C1-NHS ester (compound 8) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141159
    TCO-PEG4-acid

    PROTAC Linker Cancer
    TCO-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141166
    TCO-PEG3-NHS ester

    PROTAC Linker Cancer
    TCO-PEG3-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-133230
    Propargyl-PEG10-amine

    PROTAC Linker Cancer
    Propargyl-PEG10-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130563
    Propargyl-PEG3-CH2COOH

    PROTAC Linker Cancer
    Propargyl-PEG3-CH2COOH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-112559
    Bis-PEG2-acid

    PROTAC Linker Cancer
    Bis-PEG2-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141160
    TCO-PEG6-acid

    PROTAC Linker Cancer
    TCO-PEG6-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-115414
    Bis-propargyl-PEG8

    PROTAC Linker Cancer
    Bis-propargyl-PEG8 (compound 16e) is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130147
    Propargyl-PEG5-OH

    PROTAC Linker Cancer
    Propargyl-PEG5-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141161
    TCO-PEG8-acid

    PROTAC Linker Cancer
    TCO-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141183
    TCO-PEG4-biotin

    PROTAC Linker Cancer
    TCO-PEG4-biotin is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130374
    Propargyl-PEG8-OH

    PROTAC Linker Cancer
    Propargyl-PEG8-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-133229
    Propargyl-PEG4-alcohol

    PROTAC Linker Cancer
    Propargyl-PEG4-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130137
    m-PEG8-C10-phosphonic acid

    PROTAC Linker Cancer
    m-PEG8-C10-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141180
    TCO-PEG6-amine

    PROTAC Linker Cancer
    TCO-PEG6-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130389
    Propargyl-PEG4-O-C1-Boc

    PROTAC Linker Cancer
    Propargyl-PEG4-O-C1-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130375
    Propargyl-PEG8-Boc

    PROTAC Linker Cancer
    Propargyl-PEG7-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-117045
    Propargyl-PEG12-OH

    PROTAC Linker Cancer
    Propargyl-PEG12-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-126977
    Propargyl-PEG9-OH

    PROTAC Linker Cancer
    Propargyl-PEG9-OH is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141189
    TCO-PEG8-TCO

    PROTAC Linker Cancer
    TCO-PEG8-TCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141179
    TCO-PEG4-amine

    PROTAC Linker Cancer
    TCO-PEG4-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-120587
    Bis-PEG6-acid

    PROTAC Linker Cancer
    Bis-PEG6-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141177
    TCO-PEG2-amine

    PROTAC Linker Cancer
    TCO-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-126891
    Bis-PEG3-acid

    PROTAC Linker Cancer
    Bis-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141169
    TCO-PEG8-NHS ester

    PROTAC Linker Cancer
    TCO-PEG8-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130378
    Propargyl-PEG7-alcohol

    PROTAC Linker Cancer
    Propargyl-PEG7-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130584
    Propargyl-PEG2-Ms

    PROTAC Linker Cancer
    Propargyl-PEG2-Ms is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-114670
    Propargyl-PEG4-amine

    PROTAC Linker Cancer
    Propargyl-PEG4-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141162
    TCO-PEG12-acid

    PROTAC Linker Cancer
    TCO-PEG12-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130373
    Propargyl-PEG9-amine

    PROTAC Linker Cancer
    Propargyl-PEG9-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130819
    Tos-PEG4-THP

    PROTAC Linker Cancer
    Tos-PEG4-THP is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523).
  • HY-130380
    Propargyl-PEG7-Boc

    PROTAC Linker Cancer
    Propargyl-PEG7-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130384
    Propargyl-PEG6-Boc

    PROTAC Linker Cancer
    Propargyl-PEG6-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141188
    TCO-PEG4-TCO

    PROTAC Linker Cancer
    TCO-PEG4-TCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-113921
    m-PEG4-propargyl

    PROTAC Linker Cancer
    m-PEG4-propargyl is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-141168
    TCO-PEG6-NHS ester

    PROTAC Linker Cancer
    TCO-PEG6-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-140015
    TCO-PEG3-acid

    PROTAC Linker Cancer
    TCO-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-111875
    SNIPER(BRD)-1

    SNIPER Epigenetic Reader Domain Cancer
    SNIPER(BRD)-1, consists of an IAP antagonist LCL-161 derivative and a BET inhibitor, (+)-JQ-1, connected by a linker. SNIPER(BRD)-1 induces the degradation of BRD4 via the ubiquitin-proteasome pathway. SNIPER(BRD)-1 also degrades cIAP1 , cIAP2 and XIAP with IC50s of 6.8 nM, 17 nM, and 49nM, respectively.
  • HY-100900
    ML364

    Deubiquitinase Cancer
    ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
  • HY-P1259
    PR-39

    Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-115497
    BRD5529

    E1/E2/E3 Enzyme Inflammation/Immunology
    BRD5529 is a selective CARD9-E3 ubiquitin ligase TRIM62 protein-protein interaction inhibitor with an IC50 of 8.6 μM. BRD5529 directly and selectively binds CARD9, disrupts TRIM62 recruitment, inhibits TRIM62-mediated ubiquitinylation and activation of CARD9, and demonstrates cellular activity and selectivity in CARD9-dependent pathways.
  • HY-P1259A
    PR-39 TFA

    Proteasome Bacterial Inflammation/Immunology
    PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
  • HY-122882
    HOIPIN-8

    E1/E2/E3 Enzyme Inflammation/Immunology
    HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC.
  • HY-13811
    NSC697923

    E1/E2/E3 Enzyme Apoptosis Cancer
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
  • HY-129610
    KB02-SLF

    PROTACs FKBP Cancer
    KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF.
  • HY-128359
    ACBI1

    PROTACs Epigenetic Reader Domain Apoptosis Cancer
    ACBI1 is a potent PROTAC degrader of BAF ATPase subunits SMARCA2 and SMARCA4, also degrades the polybromo-associated BAF (PBAF) complex member PBRM1, with DC50s of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 can induce anti-proliferative effects and apoptosis.
  • HY-136528
    RA-9

    Deubiquitinase Apoptosis Cancer
    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
  • HY-103636
    PROTAC Sirt2 Degrader-1

    Sirtuin PROTACs Cancer
    PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM).
  • HY-114421
    FKBP12 PROTAC dTAG-13

    dTAG-13

    PROTACs FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader. FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-129619
    SNIPER(ER)-87

    SNIPER Estrogen Receptor/ERR Cancer
    SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
  • HY-123941
    FKBP12 PROTAC dTAG-7

    dTAG-7

    PROTACs FKBP Epigenetic Reader Domain Cancer
    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader. FKBP12 PROTAC dTAG-7 (dTAG-7) is a degrader of FKBP12 F36V with expression of FKBP12 F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-7 (dTAG-7) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN.
  • HY-130816
    (S,R,S)-AHPC-O-Ph-PEG1-NH2

    VH032-O-Ph-PEG1-NH2

    E3 Ligase Ligand-Linker Conjugate Cancer
    (S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pKD of 9.02.
  • HY-129917
    KB02-JQ1

    PROTACs Epigenetic Reader Domain Cancer
    KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
  • HY-126885
    DBCO-PEG5-NHS ester

    ADC Linker PROTAC Linker Cancer
    DBCO-PEG5-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs. DBCO-PEG5-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-126892
    Bis-PEG7-acid

    PROTAC Linker ADC Linker Cancer
    Bis-PEG7-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG6-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-130408
    m-PEG6-Amine

    ADC Linker PROTAC Linker Cancer
    m-PEG6-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG6-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-W018174
    m-PEG3-Amine

    ADC Linker PROTAC Linker Cancer
    m-PEG3-Amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. m-PEG3-Amine is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-130387
    Propargyl-PEG4-Tos

    PROTAC Linker ADC Linker Cancer
    Propargyl-PEG4-Tos is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Propargyl-PEG4-Tos is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-126894
    Bis-PEG9-acid

    PROTAC Linker ADC Linker Cancer
    Bis-​PEG9-​acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-​PEG9-​acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-118808
    Propargyl-PEG2-NHBoc

    ADC Linker PROTAC Linker Cancer
    Propargyl-PEG2-NHBoc is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-NHBoc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-126976
    Propargyl-PEG5-amine

    ADC Linker PROTAC Linker Cancer
    Propargyl-PEG5-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-126893
    Bis-PEG8-acid

    PROTAC Linker ADC Linker Cancer
    Bis-PEG8-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG8-acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-140310
    TCO-PEG4-DBCO

    ADC Linker PROTAC Linker Cancer
    TCO-PEG4-DBCO is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. TCO-PEG4-DBCO is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-W051634
    Propargyl-PEG2-amine

    ADC Linker PROTAC Linker Cancer
    Propargyl-PEG2-amine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG2-amine is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.
  • HY-130410
    Bis-PEG6-NHS ester

    ADC Linker PROTAC Linker Cancer
    Bis-PEG6-NHS ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Bis-PEG6-NHS ester is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • HY-129602
    SD-36

    PROTACs STAT Apoptosis Cancer
    SD-36 is a potent and efficacious PROTAC STAT3 degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of CRBN ligand Lenalidomide for E3 ubiquitin ligase.
  • HY-117937
    BC-1215

    Ligand for E3 Ligase Inflammation/Immunology
    BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCF Fbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.