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 [1] [2] [3] [4].
In Vitro, CCX-777 formic (20 μM; 60 min) effectively prevents the reassociation of CXCL12WT with ACKR3WT in Sf9 cells, enabling quantitative analysis of the slow dissociation half-life (102 min) of CXCL12WT from this receptor[2]. CCX-777 formic (20 μM) specifically blocks the binding of CXCL12WT to ACKR3WT in Sf9 cells[2]. CCX-777 formic (33 nM; 15 min) acts as a partial agonist for β-arrestin-2 recruitment to ACKR3 in HEK293S cells, with 52% efficacy relative to CXCL12 and a potency of [4].
References:
[1]. Santagata S, et al. CXCR4 and CXCR7 Signaling Pathways: A Focus on the Cross-Talk Between Cancer Cells and Tumor Microenvironment. Front Oncol. 2021;11:591386. Published 2021 Apr 15.
[2]. Gustavsson M, et al. Kinetics of CXCL12 binding to atypical chemokine receptor 3 reveal a role for the receptor N terminus in chemokine binding[J]. Science signaling, 2019, 12(598): eaaw3657.
[3]. Lounsbury N. Advances in CXCR7 modulators[J]. Pharmaceuticals, 2020, 13(2): 33.
[4]. Gustavsson M, et al. Structural basis of ligand interaction with atypical chemokine receptor 3. Nat Commun. 2017;8:14135. Published 2017 Jan 18.
In Vitro, CCX-777 formic (20 μM; 60 min) effectively prevents the reassociation of CXCL12WT with ACKR3WT in Sf9 cells, enabling quantitative analysis of the slow dissociation half-life (102 min) of CXCL12WT from this receptor[2]. CCX-777 formic (20 μM) specifically blocks the binding of CXCL12WT to ACKR3WT in Sf9 cells[2]. CCX-777 formic (33 nM; 15 min) acts as a partial agonist for β-arrestin-2 recruitment to ACKR3 in HEK293S cells, with 52% efficacy relative to CXCL12 and a potency of [4].
References:
[1]. Santagata S, et al. CXCR4 and CXCR7 Signaling Pathways: A Focus on the Cross-Talk Between Cancer Cells and Tumor Microenvironment. Front Oncol. 2021;11:591386. Published 2021 Apr 15.
[2]. Gustavsson M, et al. Kinetics of CXCL12 binding to atypical chemokine receptor 3 reveal a role for the receptor N terminus in chemokine binding[J]. Science signaling, 2019, 12(598): eaaw3657.
[3]. Lounsbury N. Advances in CXCR7 modulators[J]. Pharmaceuticals, 2020, 13(2): 33.
[4]. Gustavsson M, et al. Structural basis of ligand interaction with atypical chemokine receptor 3. Nat Commun. 2017;8:14135. Published 2017 Jan 18.