PROTAC Degrader

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  1. degrader

    PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC, which potently and selectively induces the degradation of Bcl-2 (IC50, 4.94 μM; DC50, 3.0 μM) and Mcl-1 (IC50, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.
  2. Mcl-1 inhibitor

    PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.
  3. MCL-1/PROTAC degrader

    dMCL1-2 is a potent and selective degrader of myeloid cell leukemia 1 (MCL1) based on PROTAC, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.
  4. PROTAC BRD4 degrader

    ZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM.
  5. ER PROTAC degrader

    ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
  6. 10-atom linker PROTAC

    SJFδ is a 10-atom linker PROTAC. SJFδ degrades p38δ with a DC50 of 46.17?nM, but does not degrade p38α, p38β, or p38γ.
  7. 13-atom linker PROTAC

    SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16??nM, but is far less effective at degrading p38δ (DC50=299?nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5??M.
  8. FLT-3 ITD degrader

    PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction.
  9. dual BRD7/9 PROTAC degrader

    VZ185 is a potent, fast, and selective dual BRD7/9 PROTAC degrader with DC50s of 4.5 and 1.8 nM, respectively.
  10. CRBN degrader

    PROTAC CRBN Degrader-1 comprises a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader.
  11. ERRa degrader

    PROTAC ERRalpha Degrader-2 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-2 is an estrogen-related receptor alpha (ERRa) degrader.
  12. ERRα Degrader

    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader.
  13. ERRα inverse agonist

    PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
  14. heterobifunctional degrader

    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader.
  15. CDK9 degrader PROTAC

    THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
  16. Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
  17. Brd4 degrader

    AT6 is a PROTAC AT1 analogue, which is a highly selective bromodomain (Brd4) degrader.
  18. TRIM24 degrader

    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
  19. AR degrader

    PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader.
  20. CRABP-II degrader

    PROTAC CRABP-II Degrader-3 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
  21. CRABP-II degrader

    PROTAC CRABP-II Degrader-2 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
  22. CRABP-II degrader

    PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
  23. Brd4 degrader

    BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
  24. BET degrader

    QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
  25. ALK PROTAC degrader

    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37?nM for binding affinity to ALK.
  26. BCL-XL degrader

    DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology.

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