PROTAC Degrader

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  1. BET degrader

    BETd-260 is a potent BET degrader based on PROTAC technology, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.
  2. BET degrader

    ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
  3. BRD4 protein degrader

    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
  4. BRD4 protein degrader

    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. ER PROTAC degrader

    ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
  10. PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
  11. BTK degrader

    MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL).
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. MDM2 degrader

    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 has the potential to be a new class of anticancer agent.
  17. BRD4-degrading PROTAC

    A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
  18. PROTAC BET degrader

    PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
  19. 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.
  20. 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.
  21. 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.
  22. 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).
  23. heterobifunctional degrader

    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader.
  24. 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).
  25. 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.
  26. BRD4BD1degrader

    dBET57 is a potent and selective degrader of BRD4BD1 based on the PROTAC technology.
  27. pVHL30 degrader

    Homo-PROTAC pVHL30 degrader 1 is a potent pVHL30 degrader based on PROTAC.
  28. BRD3/4 degrader

    MZP-55 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 8 nM for Brd4BD2.
  29. BRD3/4 degrader

    MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.
  30. TRIM24 degrader

    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
  31. 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.
  32. ERα degrader

    PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader.
  33. RAR degrader

    PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader.
  34. Sirt2 degrader

    PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide cereblon ligand for E3 ubiquitin ligase.
  35. ALK PROTAC degrader

    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37?nM for binding affinity to ALK.
  36. BCR-ABL1 tyrosine kinase degrader

    GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance.
  37. PROTAC degrader

    SNIPER(CRABP)-11, also known as PROTAC cIAP1 degrader-?4, is a potent protein degrader.

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