ap1867

AP1867 (FK506-binding protein) is a synthetic FKBP12 F36V-directed ligand attached to 320 substituted tetrahydrooxazepines (THOXs). AP1867 (FK506-binding protein) was synthesized via combined liquid- and solid-phase methods employing sequential Mitsunobu displacements followed by ruthenium-mediated olefin metathesis to close seven-membered rings; the resin-bound THOX ligands were coupled to AP1867 in parallel, yielding candidate heterodimerizers that demonstrated membrane permeability and bioactivity in human fibrosarcoma cells, facilitating the study of targeted protein interactions and intracellular modulation.

AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.

AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].

NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound that facilitates the nuclear import of cytosolic cargoes by utilizing the nuclear-localized bromodomain-containing protein 4 (BRD4) as a carrier for co-import and subsequent nuclear entrapment [1].

EB-TCIP (BAK-04-212) is a bivalent molecule composed of AP1867 and BI-3812. It facilitates the reversible formation of a ternary complex between FKBPF36V and BCL6BTB, thereby recruiting FKBP12F36V-tagged EWS/FLI1 to DNA sites bound by the transcriptional regulator BCL6, rapidly inducing expression of BCL6 target genes such as SOCS2 and CXCL11. EWS/FLI1 is a fusion transcription factor found in Ewing sarcoma. EB-TCIP is applicable for studying transcriptional dysregulation in cancer.