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PROTAC BTK degrader

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

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Screening Libraries

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157763

    PROTACs Btk Cancer
    PROTAC BTK Degrader-8 (compound 3) is a potent PROTAC BTK degrader .
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-8
  • HY-122828

    PROTACs Btk Others
    PROTAC BTK Degrader-2 is a potent BTK PROTAC degrader. PROTAC BTK Degrader-2 effectively reduces BTK protein levels .
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-2
  • HY-147943

    PROTACs Btk Cancer
    PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth . PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-1
  • HY-162280

    PROTACs RANKL/RANK Nuclear Factor of activated T Cells (NFAT) Btk Cancer
    PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-9
  • HY-153536

    PROTACs Btk Cancer
    PROTAC BTK Degrader-3 is a potent BTK degrader with a DC50 value of 10.9 nM of BTK degradation in Mino cells. PROTAC BTK Degrader-3 has the potential for B-cell malignancies, including chronic lymphoid malignancies research .
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-3
  • HY-155072

    Btk Cancer
    PROTAC BTK degraders-5(compound 3e) is a selective BTK degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research 1.
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-5
  • HY-149391

    PROTACs Btk Inflammation/Immunology
    PROTAC BTK Degrader-6 (Compound 15) is a PROTAC BTK degrader (DC50: 3.18 nM. PROTAC BTK Degrader-6 has anti-inflammatory activity, inhibits NF-κB activation, and inhibits the expression of pro-inflammatory cytokines (e.g. IL-1β, IL-6) .
    <em>PROTAC</em> <em>BTK</em> <em>Degrader</em>-6
  • HY-130982

    E3 Ligase Ligand-Linker Conjugates Cancer
    Lenalidomide-PEG3-iodine is a synthesized E3 ligase ligand-linker conjugate that incorporates the Lenalidomide based cereblon ligand and a 3-unit PEG linker. Lenalidomide-PEG3-iodine can be used in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
    Lenalidomide-PEG3-iodine
  • HY-153803

    PROTACs Molecular Glues Btk Cancer
    GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN). GBD-9 acts both as a PROTAC molecule to induce the degradation of BTK and as a molecular glue to degrade GSPT1. GBD-9 effectively inhibits cancer cell growth .
    GBD-9
  • HY-130983

    Btk Ligands for Target Protein for PROTAC Cancer
    N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
    N-piperidine Ibrutinib hydrochloride
  • HY-130504
    Propargyl-PEG1-acid
    1 Publications Verification

    PROTAC Linkers Cancer
    Propargyl-PEG1-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-CRBN PROTACs Ibrutinib(HY-10997)-based PROTAC 4 and PROTAC 5. PROTAC 5 causes the degradation of BTK and induces the degradation of CSK, LYN, and LAT2 at 10 μM . Propargyl-PEG1-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Propargyl-PEG1-acid
  • HY-130481

    PROTAC Linkers Cancer
    Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib (HY-10997)-based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells . Propargyl-PEG4-acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Propargyl-PEG4-acid
  • HY-160142

    Btk Cancer
    UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
    UBX-382
  • HY-133144

    Ligands 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) .
    Lenalidomide-OH
  • HY-154860

    PROTACs Btk Cancer
    PTD10 is a highly potent PROTAC BTK degrader (DC50: 0.5 nM, KD: 2.28 nM). PTD10 degrades BTK in Ramos and JeKo-1 cells with DC50s of 0.5 and 0.6 nM respectively. PTD10 inhibits cell growth, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 can be used for research of B-cell dysregulation .
    PTD10
  • HY-133137

    PROTACs Btk Cancer
    SJF620 is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .
    SJF620
  • HY-133137A

    PROTACs Btk Cancer
    SJF620 hydrochloride is a PROTAC connected by ligands for Cereblon and Btk with a DC50 of 7.9 nM. SJF620 contains a Lenalidomide analog for recruiting CRBN .
    SJF620 hydrochloride
  • HY-153321

    BTK-IN-24

    Btk PROTACs Inflammation/Immunology Cancer
    NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
    NX-5948
  • HY-133143

    PROTAC Linkers Cancer
    1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker. 1,2-Bis(2-iodoethoxy)ethane can be used in the synthesis of MT802 (HY-122562) and SJF620 (HY-133137). MT-802 and SJF620 are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively .
    1,2-Bis(2-iodoethoxy)ethane
  • HY-130665
    TL12-186
    1 Publications Verification

    PROTACs CDK Cancer
    TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM) .
    TL12-186

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