PROTACs

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  1. E3 ligase ligand-linker conjugate

    Pomalidomide-PEG4-Ph-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.
  2. Thalidomide-based Cereblon ligand

    Thalidomide fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1.

  3. PROTAC linker

    NH2-C2-NH-Boc (PROTAC Linker 22) is a PROTAC linker, which refers to the alkyl chain composition.NH2-C2-NH-Boc can be used in the synthesis of a series of PROTACs.
  4. 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.
  5. VHL ligand

    VL285 is a potent VHL ligand with an IC50 of 0.34 μM.
  6. PROTAC linker

    Cl-C6-PEG4-O-CH2COOH (PROTAC Linker 4) is a PROTAC linker can be used in the synthesis of chloroalkane-containing PROTACs (HaloPROTACs).
  7. PROTAC linker

    VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that incorporates the VH032 based VHL ligand and 5-unit PEG linker.
  8. PROTAC linker

    Pomalidomide-PEG4-C-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 4-unit PEG linker used in PROTAC technology.
  9. 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.
  10. BRD4 protein degrader

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

    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. ligand-linker conjugate

    CCK2R Ligand-Linker Conjugates 1 is a ligand-linker conjugate, which conjugates to the cytotoxic antimicrotubule agents Desacetyl Vinblastine Hydrazide (DAVBH) and Tubulysin B Hydrazide (TubBH) via a hydrophilic peptide linker.
  17. PROTAC linker

    Dox-Ph-PEG1-Cl (PROTAC Linker 34) is a PROTAC linker, which refers to the PEG composition. Dox-Ph-PEG1-Cl can be used in the synthesis of a series of PROTACs.
  18. Lenalidomide-based Cereblon ligand

    Lenalidomide-C5-NH2 is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-NH2 can be connected to the ligand for protein by a linker to form PROTACs.
  19. VH032-based VHL ligand

    VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1).
  20. PROTAC linker

    Boc-NH-C6-amido-C4-acid is a PROTAC linker, which refers to the alkyl/ether composition. Boc-NH-C6-amido-C4-acid can be used in the synthesis of a series of PROTACs.
  21. PEG PROTAC linker

    PEG6-(CH2CO2H)2 is a PEG derivative containing two terminal carboxylic acid groups. The hydrophilic PEG spacer increases solubility in aqueous media.
  22. PROTAC linker

    Boc-NH-PEG2-C2-amido-C4-acid (PROTAC Linker 30) is a PROTAC linker, which refers to the PEG composition. Boc-NH-PEG2-C2-amido-C4-acid can be used in the synthesis of a series of PROTACs.
  23. PROTAC linker

    NH2-Ph-C4-acid-NH2-Me (PROTAC Linker 31) is a PROTAC linker, which refers to the Alkyl-Chain composition. NH2-Ph-C4-acid-NH2-Me can be used in the synthesis of a series of PROTACs.
  24. ER PROTAC degrader

    ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
  25. 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).
  26. ABL inhibitor

    SNIPER(ABL)-062, in which an ABL inhibitor is linked to a ligand of cIAP1 via a linker containing a variable polyethylene glycol (PEG) unit, shows a potent activity to degrade the BCR-ABL protein.
  27. 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).
  28. CRBN modulator

    TD-106 is a cereblon (CRBN) modulator, which can be used for targeted protein degradation. BRD4 PROTACs with TD-106 induce BRD4 degradation.
  29. 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.
  30. 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.
  31. FBXO3 inhibitor

    BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCFFbxo3 catalyzed Fbxl2 ubiquitination.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used in PROTAC technology.
  38. E3 ligase ligand-linker conjugate

    Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology.
  39. PROTAC linker

    Bis-PEG1-C-PEG1-CH2COOH (PROTAC Linker 26) is a PROTAC linker, which refers to the PEG composition. Bis-PEG1-C-PEG1-CH2COOH can be used in the synthesis of a series of PROTACs.
  40. E3 ligase ligand-linker conjugate

    Pomalidomide-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a PEG linker used in PROTAC technology.
  41. 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.
  42. PROTAC linker

    Bis-NH2-C1-PEG3 (PROTAC Linker 24) is a PROTAC linker, which refers to the alkyl/ether composition. Bis-NH2-C1-PEG3 can be used in the synthesis of a series of PROTACs.
  43. PTK2/FAK inhibitor

    BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC.
  44. 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.
  45. 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.
  46. PROTAC linker

    Phenol-amido-C1-PEG3-N3 (PROTAC Linker 21) is a PROTAC linker, which refers to the PEG composition. Phenol-amido-C1-PEG3-N3 can be used in the synthesis of a series of PROTACs.
  47. PROTAC linker

    N3-PEG4-C2-NH2 (PROTAC Linker 20) is a polyethylene glycol (PEG)-based PROTAC linker. N3-PEG4-C2-NH2 can be used in the synthesis of a series of PROTACs.
  48. 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).
  49. PROTAC linker

    Bis-NH2-PEG2 (PROTAC Linker 19) is a PROTAC linker, which refers to the PEG composition. Bis-NH2-PEG2 can be used in the synthesis of a series of PROTACs.
  50. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 1 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 1 can be used to design SNIPERs.

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