PROTAC

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  1. ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells.
  2. VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.
  3. VHL ligand

    VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
  4. 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.
  5. BET degrader

    QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
  6. 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.
  7. BET degrader

    PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
  8. PROTAC BRD9 degrader

    PROTAC BRD9 Degrader-1 is a lead PROTAC BRD9 chemical degrader (IC50=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.
  9. Pomalidomide-PEG4-C2-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.
  10. ALK PROTAC degrader

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

    MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19?nM for binding affinity to ALK.
  12. Sirt2 inhibitor

    SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM.
  13. E3 ligase ligand-linker conjugate

    Thalidomide-O-amido-C4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  14. FKBP ligand

    SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.
  15. E3 ligase ligand-linker conjugate

    Thalidomide-O-amido-C8-NH2 TFA (Cereblon Ligand -Linker Conjugates 2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  16. PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.
  17. E3 ligase ligand-linker conjugate

    Thalidomide-O-amido-C4-NH2 TFA (Cereblon Ligand-Linker Conjugates 6 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  18. N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL.
  19. E3 ligase ligand-linker conjugate

    Thalidomide-O-amido-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
  20. PROTAC BRD9-binding moiety 1 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
  21. BRD4 inhibitor

    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
  22. (S,R,S)-AHPC-(C3-?PEG)?2-?C6-?Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-?PEG)?2-?C6-?Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
  23. E3 ligase ligand-linker conjugate

    Thalidomide-O-amido-PEG3-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
  24. (S,R,S)-AHPC-PEG6-C4-Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
  25. Thalidomide-O-amido-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  26. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
  27. E3 ligase ligand-linker conjugate

    Thalidomide-O-amido-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
  28. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-PEG2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology.
  29. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-PEG3-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
  30. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
  31. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-PEG1-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.
  32. E3 ligase ligand-linker conjugate

    (S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in PROTAC technology.
  33. Thalidomide-O-COOH (Cereblon ligand 3) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein.
  34. PROTAC linker

    Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
  35. Thalidomide-OH (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-OH (Cereblon ligand 2) can be connected to the ligand for protein by a linker to form PROTACs.
  36. Boc-C1-PEG2-C4-Cl (PROTAC Linker 1) is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.
  37. PROTAC linker

    N33-TEG-COOH is a PROTAC linker containing four polyethylene glycol (PEG) units.
  38. cereblon (CRBN) modulator

    CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
  39. CRBN modulator

    Iberdomide (CC-220) is a cereblon (CRBN) modulator with an IC50 of 60 nM.
  40. 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).
  41. 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.
  42. 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).
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

Items 51-100 of 5610

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