GLPBio

PROTAC

Read More about this category

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)

  • GC81024 structure
    GC81024PROTAC RNF4 degrader-1
    Purity: >98.00%

    PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader ( K d = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system.

  • GC81025 structure
    GC81025PSP-0119
    CAS: 3104855-98-0
    Purity: >98.50%

    PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 ( IC 50 = 2.83 nM).

  • GC81026 structure
    GC81026PROTAC SKP2 Degrader-1
    CAS: 3120650-15-6
    Purity: >99.50%

    PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a K d value of 6.28 μM.

  • GC81027 structure
    GC81027PROTAC HIF-1α degrader-2
    CAS: 3095636-64-6
    Purity: >98%

    PROTAC HIF-1α degrader-2 is a highly efficient and selective PROTAC degrader targeting HIF-1α. PROTAC HIF-1α degrader-2 promotes HIF-1α degradation via the ubiquitin-proteasome pathway by facilitating the formation of a HIF-1α/VHL ternary complex.

  • GC81036 structure
    GC81036PROTAC AAK1 degrader-1
    CAS: 3113123-63-7
    Purity: >98.00%

    PROTAC AAK1 degrader-1 (compound 14) is a selective PROTAC AAK1 degrader with a DC 50 of <10 nM.

  • GC81038 structure
    GC81038PROTAC mHTT Degrader-1
    CAS: 2919475-43-5
    Purity: >98%

    PROTAC mHTT Degrader-1 is a blood-brain barrier-penetrant mutant huntingtin ( mHTT ) PROTAC degrader.

  • GC81039 structure
    GC81039PROTAC MALT1 Degrader-1
    CAS: 2975664-37-8
    Purity: >98.00%

    PROTAC MALT1 Degrader-1 (Compound 176) is a MALT1 PROTAC degrader.

  • GC81041 structure
    GC81041GP262
    CAS: 3107761-81-6
    Purity: >98.50%

    GP262 is a PI3K/mTOR PROTAC degrader targeting PI3Kγ, PI3Kα and mTOR with DC 50 values of 42.23 nM, 227.4 nM and 45.4 nM, respectively in MDA-MB-231 cells.

  • GC81296 structure
    GC81296PRT3789 epimer
    CAS: 3023568-80-8
    Purity: >98.50%

    PRT3789 epimer is an epimer of PRT3789.

  • GC81297 structure
    GC81297DFCI-002-06
    CAS: 3092208-36-8
    Purity: >98%

    DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively.

  • 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.