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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)

  • GC73489 structure
    GC73489PROTAC Her3 Degrader-8
    CAS: 2103331-95-7
    Purity: >99.00%

    PROTAC Her3 Degrader-8 (Compound PP2) is a PROTAC that can degrade Her3 protein in vitro and cell experiments, and can be used to study diseases regulated by HER family proteins.

  • GC73490 structure
    GC73490GBD-9
    CAS: 2864408-92-2
    Purity: >98.00%

    GBD-9 is a double-mechanism degrader that efficiently degrades BTK and GSPT1 by recruiting the E3 ligase cereblon (CRBN).

  • GC73493 structure
    GC73493PROTAC KRAS G12C degrader-2
    CAS: 2378257-72-6
    Purity: >98.00%

    PROTAC KRAS G12C degrader-2 (compound 432) is a modulator of K-Ras protein drolysis.

  • GC73506 structure
    GC73506PROTAC EGFR degrader 8
    CAS: 2925923-46-0
    Purity: >98.00%

    PROTAC EGFR degrader 8 (T-184) is a PROTAC EGFR degrader.

  • GC73536 structure
    GC73536JET-209
    Purity: >98.00%

    JET-209 is a potent PROTAC CBP/p300 degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300.

  • GC73547 structure
    GC73547PROTAC TG2 degrader-2
    Purity: >99.00%

    PROTAC TG2 degrader-2 (compound 7) is a selective, competitive degrader targeting Transglutaminase 2 (TG2), with Kd > 100 μM.

  • GC73550 structure
    GC73550JH-XII-03-02
    CAS: 2415900-86-4
    Purity: >99.00%

    JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader.

  • GC73570 structure
    GC73570PROTAC BRD9 Degrader-7
    Purity: >99.00%

    PROTAC BRD9 Degrader-7 is an orally active and selective degrader of BRD9 with a DC50 of 1.02 nM.

  • GC73606 structure
    GC73606PIK5-12d
    Purity: >99.00%

    PIK5-12d is a PROTAC PIKfyve degrader (DC50: 1.48 nM).

  • GC73613 structure
    GC73613ARD-1676
    CAS: 2632305-36-1
    Purity: >99.00%

    ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand.

  • GC73615 structure
    GC73615CARM1 degrader-1 hydrochloride

    CARM1 degrader-1 drochloride is the drochloride salt form of CARM1 degrader-1.

  • GC73660 structure
    GC73660SMD-3040
    CAS: 3033109-92-8
    Purity: >99.00%

    SMD-3040 is a potent and selective of SMARCA2 PROTAC degrader (DC50: 12 nM).

  • GC73661 structure
    GC73661SMD-3040 TFA
    Purity: >99.00%

    SMD-3040 TFA is a selective degrader of SMARCA2.

  • GC73728 structure
    GC73728PROTAC EZH2 Degrader-2
    Purity: >99.00%

    PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand.

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

    ACBI3 is a selective pan-KRAS degrader (PROTAC), composed of a target protein ligand (pan-KRAS degrader 1, used to bind KRAS protein), an E3 ligase ligand (E3 ligase Ligand 43, used to recruit the VHL E3 ubiquitin ligase complex), and a linker (1-Bromo-4-(ethynyloxy)butane, used to optimize spatial conformation).

  • GC73764 structure
    GC73764NUCC-0226272
    CAS: 3004503-12-9
    Purity: >98.00%

    NUCC-0226272 is a potent PROTAC that targets EZH2 for degradation.

  • GC73786 structure
    GC73786ARV-393
    CAS: 2851885-95-3
    Purity: >98.00%

    ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6.

  • GC73800 structure
    GC73800MS181
    Purity: >98.00%

    MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader.

  • GC73819 structure
    GC73819PROTAC BET Degrader-12
    Purity: >98.00%

    PROTAC BET Degrader-12 (Compound 8b) is a PROTAC degrader for bromodomain and extra-terminal domain (BET)-containing proteins, which degrades the BRD3 and BRD4 in a DCAF11-dependent manner.

  • GC73868 structure
    GC73868WD6305 TFA
    Purity: >98.00%

    WD6305 TFA is a potent METTL3-targeted PROTAC degrader.

  • GC73871 structure
    GC73871INY-05-040
    CAS: 2503018-29-7
    Purity: >98.00%

    INY-05-040 is a AKT degrader that can selectively and quickly degrade all three AKT isoforms.

  • GC73881 structure
    GC73881PRO-6E
    CAS: 2353493-69-1
    Purity: >99.00%

    PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells.

  • GC73929 structure
    GC73929MG degrader 1
    Purity: >99.00%

    MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC50 value of 1.385 nM in MM.1S cells.

  • GC73956 structure
    GC73956LLC0424
    Purity: >98.00%

    LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader.