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PROTAC

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PROTACs or Proteolysis Targeting Chimeric Molecules are heterobifunctional nanomolecules that theoretically target any protein for ubiquitination and degradation. In terms of the structure, PROTACs consist of one moiety which is recognized by the E3 ligase. This moiety is then chemically and covalently linked to a small molecule or a protein that recognizes the target protein. The trimeric complex formation leads to the transfer of ubiquitins to the target protein.

By removing target proteins directly rather than merely blocking them, PROTACs can provide multiple advantages over small molecule inhibitors, which can require high systemic exposure to achieve sufficient inhibition, often resulting in toxic side effects and eventual drug resistance. PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins, thus can be directly applied to cells or injected into animals without the use of vectors.

Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases, such as cancer, driven by the aberrant expression of a disease-causing protein. In addition to the use of PROTACs for the treatment of human disease, these molecules provide a chemical genetic approach to “knock down” proteins to study their function. Currently, there are several small molecule inhibitors that have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc.

References:

[1] Sakamoto KM. Pediatr Res. 2010 May;67(5):505-8.

[2] Neklesa TK, et al. Pharmacol Ther. 2017 Jun;174:138-144.

Research Areas

Products Related to PROTAC(296)

  • GC69745 structure
    GC69745PROTAC BRD4 Degrader-11
    Purity: >98%

    PROTAC BRD4 Degrader-11 (composé 9a) est un PROTAC efficace qui relie le ligand von Hippel-Lindau et le ligand BRD4. Le PROTAC BRD4 Degrader-11 peut dégrader la protéine BRD4 dans les cellules cancéreuses de la prostate PC3 en se liant aux anticorps STEAP1 et CLL1, avec des valeurs DC50 respectives de 0,23 nM et 0,38 nM.

  • GC69746 structure
    GC69746PROTAC BRD9 Degrader-4
    CAS: 2633632-34-3
    Purity: >98%

    PROTAC BRD9 Degrader-4 est un dégradeur bifonctionnel de BRD9 étudié pour le traitement du cancer.

  • GC69748 structure
    GC69748PROTAC CDK12/13 Degrader-1 TFA
    Purity: >98%

    PROTAC CDK12/13 Degrader-1 (7f) TFA est un dégradeur doublement sélectif et efficace de la kinase cycline-dépendante CDK12/CDK13, avec des valeurs DC50 respectives de 2,2 nM et 2,1 nM. PROTAC CDK12/13 Degrader-1 TFA possède une activité anti-proliférative et peut être utilisé dans la recherche sur le cancer du sein.

  • GC69749 structure
    GC69749PROTAC CYP1B1 degrader-1
    CAS: 2411389-67-6
    Purity: >98.00%

    PROTAC CYP1B1 degrader-1 (Composé 6C) est un dérivé d'α-naphtoflavone qui peut éliminer la résistance médiée par le cytochrome P450 (CYP) 1B1 en ciblant sa dégradation via PROTAC. Les IC50 pour CYP1B1 et CYP1A2 sont respectivement de 95,1 et 9838,6 nM. PROTAC CYP1B1 Degrader-1 peut être utilisé pour étudier le cancer de la prostate avec surexpression de CYP1B1.

  • GC69750 structure
    GC69750PROTAC IRAK3 degrade-1 formic
    Purity: >98.00%

    PROTAC IRAK3 degrade-1 (composé 23) formique est un dégradeur sélectif et efficace d'IRAK3 (IC50 = 5 nM).

  • GC69951 structure
    GC69951SS47 TFA
    Purity: >99.00%

    SS47 TFA est un dégradeur de HPK1 basé sur PROTAC, qui peut induire la dégradation de HPK1 médiée par le protéasome. SS47 TFA dégrade HPK1 et améliore considérablement l'efficacité anti-tumorale in vivo des cellules CAR-T BCMA. HPK1 est une kinase régulatrice d'immunosuppression et constitue une cible potentielle pour l'immunothérapie du cancer.

  • GC70162 structure
    GC70162YX-2-107
    CAS: 2417408-46-7
    Purity: >99.00%

    YX-2-107 est un PROTAC qui dégrade sélectivement CDK6 (IC50= 4,4 nM). En vitro, YX-2-107 inhibe efficacement la phosphorylation de RB et l'expression de FOXM1, ainsi que le développement d'une ALL Ph+ chez des rats. YX-2-107 peut être utilisé dans la recherche sur la leucémie lymphoblastique aiguë (ALL) à chromosome Philadelphie positif (Ph+).

  • GC73732 structure
    GC73732ACBI3
    CAS: 2938169-76-5
    Purity: >98.00%

    ACBI3 (composé 7) est un dégradeur pan-KRAS.

  • 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 ).