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. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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).
  9. 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.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 3 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 3 can be used to design SNIPERs.
  28. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 5 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 5 can be used to design SNIPERs.
  29. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 12 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 12 can be used to design SNIPERs.
  30. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 2 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 2 can be used to design SNIPERs.
  31. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 14 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 14 can be used to design SNIPERs.
  32. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 15 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 15 can be used to design SNIPERs.
  33. PROTAC linker

    cIAP1 Ligand-Linker Conjugates 11 incorporates an IAP ligand for the E3 ubiquitin ligase, and a PROTAC linker. cIAP1 Ligand-Linker Conjugates 11 can be used to design SNIPERs.
  34. E3 ubiquitin ligase ligand

    E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  35. E3 ubiquitin ligase ligand

    E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
  36. E3 ubiquitin ligase ligand

    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs.
  37. PROTAC linker

    Tos-PEG3-NH-Boc (PROTAC Linker 9) is a PROTAC linker, which refers to the PEG composition. Tos-PEG3-NH-Boc can be used in the synthesis of a series of PROTACs.
  38. PROTAC linker

    PEG3-O-CH2COOH (Compound 15b) is a PROTAC linker can be used in the synthesis of a series of SNIPER(ER)s.
  39. PROTAC linker

    Tos-PEG4-NH-Boc (PROTAC Linker 7) is a PROTAC linker, which refers to the PEG composition. Tos-PEG4-NH-Boc can be used in the synthesis of a series of PROTACs.
  40. PROTAC linker

    Tos-PEG3-O-C1-CH3COO (PROTAC Linker 6) is a PROTAC linker, which refers to the PEGs composition.
  41. heterobifunctional degrader

    FKBP12 PROTAC dTAG-7 (dTAG-7) is a heterobifunctional degrader.
  42. 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).
  43. E3 ligase ligand-linker conjugate

    Pomalidomide-PEG3-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
  44. FKBP ligand

    AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.
  45. TRIM24 degrader

    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
  46. SNIPER inhibitor

    SNIPER(BRD4)-1 is a specific and nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPER) which acts as a protein degradation inducer of bromodomain-containing protein 4 (BRD4).
  47. SNIPER(ABL)-039, conjugating Dasatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 nM. IC50s are 0.54 nM, 10 nM, 12 nM, and 50 nM for ABL, cIAP1, cIAP2, XIAP, respectively.
  48. SNIPER(ABL)-033, conjugating HG-7-85-01 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 0.3 μM.
  49. SNIPER(ABL)-024, conjugating GNF5 (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 5μM.
  50. SNIPER(ABL)-058, conjugating Imatinib (ABL inhibitor) to LCL161 derivative (IAP ligand) with a linker, induces the reduction of BCR-ABL protein with a DC50 of 10 μM.

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