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PROTAC

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The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.

PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.

Products Related to PROTAC(273)

  • GC73996 structure
    GC73996PROTAC AR/AR-V7 degrader-1
    CAS: 2841308-96-9
    Purity: >98.00%

    PROTAC AR/AR-V7 degrader-1（27 c）は、PROTACベースのデュアルAR AR−V 7分解器であり、ARとAR−V 7のDC 50値はそれぞれ2.67と2.64μMである。

  • GC74013 structure
    GC74013FOSL1 degrader 1

    FOSL1 degrader 1(4)はt-5224-protacの一種であり、hnsccにおいてfosl1 (ap-1)を特異的に分解し、がん幹性遺伝子発現を抑制する。

  • GC74027 structure
    GC74027DAS-5-oCRBN
    Purity: >98.00%

    DAS-5-oCRBNはc-Srcキナーゼの選択性と強力なPROTAC分解剤である。

  • GC74035 structure
    GC74035AU-24118
    Purity: >98.00%

    AU-24118はmSWI/SNF ATP酵素（SMARCA 2とSMARCA 4）とPBRM 1の経口生物学的に利用可能なタンパク質加水分解ターゲットブロック（PROTAC）分解剤である。

  • GC74044 structure
    GC74044ARM165
    Purity: >99.00%

    ARM165は異二官能分子である。

  • GC74050 structure
    GC74050PROTAC CDK4/6 degrader 1
    CAS: 3025082-14-5
    Purity: >98.00%

    PROTAC CDK4/6 degrader 1（化合物7 f）はCDK 4とCDK 6の二重分解剤であり、DC 50はそれぞれ10.5と2.5 nMである。

  • GC74412 structure
    GC74412xStAx-VHLL TFA
    Purity: >99.00%

    xStAx-VHLL TFA、β-cateninの分解を維持し、Wnt信号伝導への強い抑制を示すPROTAC。β−catenin汎素化を促進する。

  • GC79180 structure
    GC79180YZ-836P
    CAS: 3086041-35-9
    Purity: >98.00%

    YZ-836P is a Protein arginine methyltransferase 5 ( PRMT5 ) targeting agent.

  • GC79419 structure
    GC79419PROTAC BCL6 Degrader-2
    Purity: >99.50%

    PROTAC BCL6 Degrader-2 is an orally active, selective BCL6 PROTAC degrader ( DC 50 : 0.45 nM in HEK293T cells).

  • GC80853 structure
    GC80853(4R,5S)-YX-02-030
    CAS: 3049077-01-9
    Purity: >99.50%

    (4R,5S)-YX-02-030 is an isomer of YX-02-030.

  • GC80856 structure
    GC80856(R,R)-Bexobrutideg
    CAS: 2649400-33-7
    Purity: >98.50%

    (R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg.

  • GC80875 structure
    GC80875PROTAC survivin degrader-1
    CAS: 3079079-69-6
    Purity: >98%

    PROTAC survivin degrader-1 is an orally active, CNS-penetrant survivin -targeting PROTAC.

  • GC80876 structure
    GC80876G9D-4 TFA
    Purity: >99.00%

    G9D-4 TFA is a G9a PROTAC degrader.

  • GC80877 structure
    GC80877LD-110 triTFA
    Purity: >99.50%

    LD-110 triTFA is a highly efficient and effective LSD1 PROTAC degrader ( DC 50 = 0.44 μM).

  • GC80880 structure
    GC80880dCASP1-55
    Purity: >98%

    dCASP1-55 is a cereblon-dependent caspase-1 ( CASP1 ) PROTAC degrader.

  • GC80881 structure
    GC80881PROTAC DAPK1 Degrader-1
    CAS: 3063030-38-3
    Purity: >96.50%

    PROTAC DAPK1 Degrader-1 is a death-associated protein kinase 1 (DAPK1) degrader with a DC 50 of 119.6 nM.

  • GC80884 structure
    GC80884CXJ2080
    Purity: >98%

    CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC 50 of 0.88 nM.

  • GC80885 structure
    GC80885PROTAC CDK6 Degrader 1
    Purity: >98.50%

    PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC 50 of 0.037 μM.

  • GC80886 structure
    GC80886PROTAC CDK2/4/6 Degrader-2
    CAS: 2541626-49-5
    Purity: >97.00%

    PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader.

  • GC80887 structure
    GC80887MA203
    Purity: >98%

    MA203 is a selective CHK1 PROTAC degrader.

  • GC80888 structure
    GC80888PROTAC PLK1 Degrader-2
    Purity: >99.00%

    PROTAC PLK1 Degrader-2 is a peptide-based N-end rule PLK1 mini-PROTAC.

  • GC80889 structure
    GC80889PROTAC HDAC4 Degrader-2
    CAS: 3035189-46-6
    Purity: >98%

    PROTAC HDAC4 Degrader-2 is a class IIa selective negative control for HDAC4 PROTAC degraders, with an IC 50 of 0.15 μM against HDAC4 and a cellular IC 50 of 0.18 μM.

  • GC80893 structure
    GC80893PROTAC CDK2/4 Degrader-1
    Purity: >98.00%

    PROTAC CDK2/4 Degrader-1 is a PROTAC degrader of cyclin-dependent kinase 2 ( CDK2 ) and cyclin-dependent kinase 4 ( CDK4 ).

  • GC80894 structure
    GC80894(S)-JWZ-5-13
    Purity: >99.50%

    (S)-JWZ-5-13 (compound 17-Neg), a PROTAC CDK7 degrader, is a negative control compound of JWZ-5-13.