XY-52 (Compound 32), an ST2 (Stimulation-2) inhibitor, exhibits IC50 values of 5.68 μM and 4.59 μM in the AlphaLISA and HEK-Blue assays, respectively. It promotes proinflammatory T-cell proliferation and diminishes plasma sST2 and IFNγ biomarkers in a graft versus host disease (GVHD) mouse model [1].

XY1 is a very close analogue of SGC707 (a potent, selective, and non-competitive inhibitor of PRMT3 with IC50 of 31 nM), It is intended to be used as a negative control for SGC707 in studies involving PRMT3 action.

XY-4, a derivative of 1-palmitoyl lysophosphatidic acid (1-palmitoyl LPA094) and an agonist of peroxisome proliferator-activated receptor γ (PPARγ), effectively induces reporter gene expression in RAW 264.7 macrophages harboring a peroxisome proliferator-response element (PPRE) at a concentration of 5 µM. Unlike its action on PPARγ, XY-4 does not serve as an agonist for lysophosphatidic acid receptor 1 (LPA1), LPA2, or LPA3. Furthermore, at a lower concentration of 1 µM, it promotes platelet aggregation in vitro and triggers carotid artery neointima formation in rats.

XY-06-007, a potent and selective bump-and-hole (B&H) PROTAC BRD4 BD1 L94V degrader, exhibits a DC50, 6 h of 10 nM specifically against BRD4 BD1 L94V without degrading off-targets. It also demonstrates favorable pharmacokinetics for in vivo studies [1].