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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(305)

  • 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: >98.00%

    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: >98.00%

    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: >98.00%

    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: >98.00%

    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: >98.00%

    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.

  • GC91440 structure
    GC91440Dth
    Purity: >95.00%

    Dth is a proteolysis-targeting chimera (PROTAC) composed of the fluorescent probe for RNA DFHBI and the immunomodulatory compound thalidomide .

  • GC91442 structure
    GC91442C-02
    Purity: >95.00%

    C-02 is a proteolysis-targeting chimera (PROTAC) composed of the hexokinase inhibitor lonidamine linked to the cereblon ligand thalidomide .

  • GC91582 structure
    GC91582Pomalidomide 4'-PEG5-amine (hydrochloride)
    CAS: 2357117-23-6
    Purity: >95.00%

    Pomalidomide 4’-PEG5-amine is a PEGylated form of the cereblon (CRBN) inhibitor pomalidomide .

  • GC91584 structure
    GC91584Pomalidomide 4'-alkylC6-amine (hydrochloride)
    CAS: 2375194-37-7
    Purity: >98.00%

    Pomalidomide 4'-alkylC6-amine is a building block in the synthesis of proteolysis-targeting chimeras (PROTACs) and a derivative of the cereblon inhibitor pomalidomide .

  • GC91586 structure
    GC91586PROTAC RAF Degrader 1
    CAS: 2413035-41-1
    Purity: >98.00%

    PROTAC RAF degrader 1 is a proteolysis-targeting chimera (PROTAC) that contains the inhibitor of mutant V600E and wild-type B-RAF vemurafenib (PLX4032; ) conjugated to VHL ligand 1 .

  • 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).