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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(285)

  • GC81298 structure
    GC81298BSJ-05-037
    CAS: 2756388-01-7
    Purity: >99.50%

    BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines.

  • GC81300 structure
    GC81300PROTAC DYRK2 degrader-2
    CAS: 3061366-74-0
    Purity: >98.00%

    PROTAC DYRK2 degrader-2 is a PROTAC DYRK2 degrader based on curcumin analog A3.

  • GC81301 structure
    GC81301BSJ-04-146
    CAS: 2414478-45-6
    Purity: >98%

    BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase ( FAK ) inhibitor( IC 50 = 26 nM).

  • GC81303 structure
    GC81303PROTAC AR Degrader-12
    Purity: >98.50%

    PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS).

  • GC81459 structure
    GC81459WZS0347
    Purity: >99.00%

    WZS0347 is a MITF PROTAC degrader.

  • GC81460 structure
    GC81460BTX-6654 formate
    Purity: >98.50%

    BTX-6654 formate is a SOS1 PROTAC degrader.

  • GC81461 structure
    GC81461FPP29
    Purity: >99.00%

    FPP29 is a potent peptide-based FOXM1 PROTAC degrader.

  • GC81512 structure
    GC81512dCDK9-202
    Purity: >98.50%

    dCDK9-202 is a CDK9 PROTAC degrader with a DC 50 of 3.5 nM.

  • GC81514 structure
    GC81514PROTAC SMARCA2 degrader-35
    CAS: 3032998-97-0
    Purity: >98%

    PROTAC SMARCA2 degrader-35 (Compound 43) is a selective SMARCA2 PROTAC degrader with a DC 50 < 0.1 μM for SMARCA2.

  • GC81522 structure
    GC81522WWZ-11-098
    Purity: >98.00%

    WWZ-11-098 is a selective CDK6 PROTAC degrader with DC 50 of 2.6 nM.

  • GC81637 structure
    GC81637EBET-1593
    CAS: 3031540-97-0
    Purity: >98%

    EBET-1593 is a BET PROTAC degrader.

  • GC81638 structure
    GC81638PROTAC GPX4 degrader-5
    CAS: 3119292-91-7
    Purity: >95.00%

    PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader ( DC 50 = 28 nM).

  • GC81639 structure
    GC81639SH-26
    Purity: >98%

    SH-26 is a PHD1 PROTAC degrader with DC 50 s of 1.06 μM, 4.16 μM and 4.91 μM in MDA-MB-231, HepG2 and HEK-293T cells, respectively.

  • GC81720 structure
    GC81720DDO3602
    Purity: >98%

    DDO3602 is a PARP1 HSPTAC ( HSP90 -mediated proteolysis-targeting chimera) degrader, with a DC 50 of 490.3 nM against PARP1; its K d values for PARP1 and HSP90 are 66.5 nM and 1.64 nM, respectively.

  • GC81732 structure
    GC81732iAfaPhos1
    Purity: >98%

    iAfaPhos1 is a FKBP12F36V epimer ligand.

  • GC81862 structure
    GC81862YJ1206 TFA
    Purity: >98.00%

    YJ1206 TFA is an orally active selective CDK12 / CDK13 PROTAC degrader.

  • GC81882 structure
    GC81882PROTAC CARM1 degrader-1 TFA
    Purity: >98.00%

    PROTAC CARM1 degrader-1 TFA is a highly selective CARM1 PROTAC degrader, with a DC 50 of 8.1 nM in MCF‑7 cells.

  • GC91040 structure
    GC91040AP-1
    Purity: >95.00%

    ALKの分解を促進するPROTAC

  • GC91041 structure
    GC91041Soluble Epoxide Hydrolase PROTAC 1a
    Purity: >95.00%

    sEHの分解を促進するPROTAC

  • GC91060 structure
    GC91060Ferritin PROTAC DeFer-2
    Purity: >98.00%

    フェリチンの分解を促進するPROTAC

  • GF04054 structure
    GF04054PROTAC CDK9 degrader-4
    CAS: 2411021-01-5
    Purity: >95.00%

    PROTAC CDK9 degrader-4 is a PROTAC protein degrader that targets CDK9 (cyclin-dependent kinase 9).