FKBP12 ligand-3

FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels[1].

Product Specifications

CAS Number

[3036374-26-9]

UNSPSC

12352005

Target

FKBP

Related Pathways

Apoptosis; Autophagy; Cell Cycle/DNA Damage; Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(N([C@@H](C)C1=NC=CC=C1)C[C@@H]2COCC#C)[C@@]3([H])N([C@]2([H])CCC3)S(C4=CC(Cl)=CC(Cl)=C4)(=O)=O

Molecular Formula

C25H27Cl2N3O4S

Molecular Weight

536.47

References & Citations

[1]Bulldan A, et al. Heterobifunctional Protein Binders Enable Cell Type-Specific Killing Through In-cell Enrichment. bioRxiv, 2025: 2025.05. 16.654562.