XY221

XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2) . XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity [1].

Product Specifications

UNSPSC

12352005

Target

AMPK; Apoptosis; Bcl-2 Family; c-Myc; Epigenetic Reader Domain; PAK

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton; Epigenetics; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C1C2=C(OC(C3=C(COC)N=C(CC)N3)=C2)C(C4=CC(C(C)(O)C)=CC=C4OC5=C(C)C=C(F)C=C5C)=CN1C

Molecular Formula

C32H34FN3O5

Molecular Weight

559.63

References & Citations

[1]Tong JB, et al. Discovery of novel BRD4-BD2 inhibitors via in silico approaches: QSAR techniques, molecular docking, and molecular dynamics simulations. Mol Divers. 2024 Apr;28 (2) :671-692.