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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)

  • 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.

  • GC80895 structure
    GC80895PROTAC USP39 Degrader-1
    Purity: >98.00%

    PROTAC USP39 Degrader-1 is a USP39 PROTAC degrader with K d values of 136 nM and 232 nM, and a DC 50 value of 1.06 nM (24 h).

  • GC80896 structure
    GC80896PROTAC D16-M1P2
    Purity: >98%

    PROTAC D16-M1P2 is an orally active CRBN -mediated selective PKMYT1 PROTAC degrader, with a DC 50 of 0.7 nM in CCNE1-amplified HCC1569 breast cancer cells.

  • GC80916 structure
    GC80916ZX079
    CAS: 3124583-65-6
    Purity: >98%

    ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC 50 value of 0.035 nM and a CBP DC 50 value of < 0.02 nM.

  • GC80917 structure
    GC80917LD-110 trihydrochloride
    Purity: >98.00%

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

  • GC80918 structure
    GC80918dCBP-30
    Purity: >98%

    dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC 50 values of 0.05 nM (CBP) and 0.04 nM (p300), respectively.

  • GC80920 structure
    GC80920PROTAC PARP2 degrader-1
    CAS: 2925182-32-5
    Purity: >95.50%

    PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC 50 of 2 μM.

  • GC80921 structure
    GC80921CCT400028
    Purity: >98.00%

    CCT400028 is a PROTACs -class degrader that targets the Aurora A (AURKA) kinase.

  • GC80922 structure
    GC80922PROTAC HDAC6 degrader 7
    Purity: >98%

    PROTAC HDAC6 degrader 7 is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 ( HDAC6 ) ( IC 50 = 118 nM).

  • GC80923 structure
    GC80923PROTAC HDAC degrader-2 TFA
    Purity: >96.50%

    PROTAC HDAC degrader-2 TFA is a selective class IIb dual histone deacetylase ( HDAC6 and HDAC10 ) PROTAC degrader, with DC 50 values of 13 nM and 29 nM against HDAC6 and HDAC10, respectively.

  • GC80924 structure
    GC80924iVeliparib-AP6
    CAS: 2472645-27-3
    Purity: >98%

    iVeliparib-AP6 is a proteolysis-targeting chimera ( PROTAC ) molecule designed based on Veliparib, which targets PARP1/2.