CXCR Agonist

ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs).

LIH383 TFA is an agonist of ACKR3 (CXCR7) (EC₅₀=0.61 nM). LIH383 TFA efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.

VUF 11222 (Compound 38) is a CXCR3 non-peptide-like agonist. VUF 11222 can be used in the study of inflammation.

CCX-777 formic is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 formic induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 formic functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 formic is widely used in cancer-related research.

ACKR3 agonist 1 (compound 27) is a selective ACKR3 agonist (EC₅₀=69 nM, E_max=82%) that inhibits platelet aggregation. ACKR3 agonist 1 is metabolically stable and non-cytotoxic, and has the potential to inhibit platelet-mediated thrombosis.

CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12.

trans-VUF25471 (Compound trans-3e) is a photoswitchable ACKR3 agonist. trans-VUF25471 binds and activates ACKR3 at 10-fold lower concentrations compared to its cis-isomer.

LIH383 is an agonist of ACKR3 (CXCR7) (EC₅₀=0.61 nM). LIH383 efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling.