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)

  • GC71231 structure
    GC71231NX-5948
    CAS: 2649400-34-8
    Purity: >98.00%

    NX-5948 is an orally active proteolytic targeting chimera (PROTAC) that is a Bruton’s tyrosine kinase (BTK) degrader.

  • GC71376 structure
    GC71376SNX7886
    CAS: 2924557-42-4
    Purity: >99.00%

    SNX7886 is a potent protac degrader of CDK8/19.

  • GC71386 structure
    GC71386SMD-3040 formate
    Purity: >99.00%

    SMD-3040 formate is a potent and selective smarca2 protac degrader with strong in vivo antitumor activity.

  • GC71400 structure
    GC71400HJM-561
    CAS: 2570251-68-0
    Purity: >98.00%

    HJM-561 is a potent, selective, orally bioavailable EGFR PROTAC.

  • GC72765 structure
    GC72765Tz-Thalidomide
    CAS: 2087490-42-2
    Purity: >98.00%

    Tz-Thalidomide is a tetrazine tagged Thalidomide (Ligands for E3 Ligase).

  • GC72849 structure
    GC72849rel-PROTAC PARP1 degrader
    Purity: >98.00%

    rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader.

  • GC72850 structure
    GC72850ARD-69
    CAS: 2316837-10-0
    Purity: >99.00%

    ARD-69 (compound 34) is a potent PROTAC androgen receptor degrader.

  • GC72863 structure
    GC72863PZ703b TFA
    Purity: >98.00%

    PZ703b TFA is a Bcl-xl PROTAC degradation agent that induces apoptosis and inhibits cancer cell proliferation for bladder cancer research.

  • GC72864 structure
    GC72864PZ703b hydrochloride
    Purity: >99.00%

    PZ703b drochloride is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation.

  • GC73005 structure
    GC73005SJF-1528 hemihydrate
    Purity: >98.00%

    SJF-1528 hemidrate is the hemidrate form of SJF-1528.

  • GC73043 structure
    GC73043QC-01-175
    CAS: 2267290-96-8
    Purity: >98.00%

    QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau.

  • GC73046 structure
    GC73046AZ'6421
    CAS: 2361115-35-5
    Purity: >98.00%

    AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha.

  • GC73053 structure
    GC73053BSJ-03-204 triTFA
    Purity: >99.00%

    BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK.

  • GC73096 structure
    GC73096PF15 TFA
    Purity: >99.00%

    PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN.

  • GC73101 structure
    GC73101(4S)-PROTAC SOS1 degrader-1 diTFA
    Purity: >98.00%

    (4S)-PROTAC SOS1 degrader-1 (diTFA) is a potent PROTAC SOS1 degrader.

  • GC73110 structure
    GC73110PROTAC SOS1 degrader-1 TFA
    Purity: >99.00%

    PROTAC SOS1 degrader-1 (TFA) is a potent PROTAC SOS1 degrader with an DC50 of 98.4 nM.

  • GC73112 structure
    GC73112JPS014 TFA
    Purity: >98.00%

    JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC).

  • GC73113 structure
    GC73113JPS016 TFA
    Purity: >98.00%

    JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC).

  • GC73124 structure
    GC73124dTAG-47-NEG
    Purity: >97.00%

    dTAG-47-NEG is an analog of dTAG-47 that cannot bind and recruit cereblon (CRBN). dTAG-47-NEG can be used as a heterobifunctional negative control of dTAG-47.

  • GC73129 structure
    GC73129SIAIS164018 hydrochloride
    Purity: >99.00%

    SIAIS164018 drochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively.

  • GC73139 structure
    GC73139SJ1008030 formic
    Purity: >97.00%

    SJ1008030 (compound 8) formic is a JAK2 PROTAC which selectively degrades JAK2.

  • GC73142 structure
    GC73142PROTAC EGFR degrader 7 diTFA
    Purity: >99.00%

    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13.2 nM.

  • GC73143 structure
    GC73143MS9449
    CAS: 2772612-96-9
    Purity: >98.00%

    MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively.

  • GC73147 structure
    GC73147XL01126
    CAS: 3011029-58-3
    Purity: >99.00%

    XL01126 is a potent LRRK2 PROTAC (DC50: 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2)) composed of the VHL ligand VH 101, thiol and the LRRK2 inhibitor HG-10-102-01.