PROTAC

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  1. Ubiquitin ligase inducer

    Lenalidomide is a derivative of thalidomide. In vitro, lenalidomide has three main activities: direct anti-tumor effect, inhibition of the micro environment support for tumor cells, and immunomodulatory role. It induces tumor cell apoptosis directly and indirectly by inhibition of bone marrow stromal cell support, by anti-angiogenic and anti-osteoclastogenic effects, and by immunomodulatory activity.
  2. 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.
  3. Cyclosporin A (Cyclosporine A) is an immunosuppressant agent widely used in post-allogeneic organ transplant to reduce the activity of the immune system.
  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. 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.
  11. 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.

  12. 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.
  13. MZ1

    BRD4 protein degrader

    MZ1 is a potent inducer of reversible, long-lasting and selective removal of BRD4 over BRD2 and BRD3.
  14. 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.
  15. 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.
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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).
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. ER PROTAC degrader

    ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
  27. TRIM24 degrader

    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
  28. 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).
  29. 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.
  30. (S,R,S)-AHPC TFA (MDK7526 TFA) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA (MDK7526 TFA) can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
  31. 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.
  32. 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.
  33. 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.
  34. Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .
  35. MV-1-NH-Me, the MV-1 based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
  36. GNF5-amido-Me, the GNF5 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
  37. Bestatin-amido-Me, the Bestatin-based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
  38. Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.
  39. 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.
  40. androgen ligand

    Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.
  41. 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.
  42. BI-3802 is a highly potent BCL6 degrader, inhibiting the BTB domain of BCL6, with an IC50 of ??3 nM; BI-3802 has antitumor activity.
  43. estrogen ligand

    Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
  44. 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.
  45. CRABP-II degrader

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

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

    PROTAC CRABP-II Degrader-1 is a potent cellular retinoic acid binding protein (CRABP-II) degrader based on cIAp1.
  48. 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.
  49. 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.
  50. VHL ligand

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

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