Biological Activity
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM; MSX-122 has anti-inflammatory and anti-metastatic activity.
In Vitro
MSX-122 is a partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 shows no inhibition on cAMP reduction mediated by their corresponding ligands CCR3/CCL5 and CCR5/CCL5. MSX-122 (100 nM) potently blocks invasion of 78% MDA-MB-231 cells. However, MSX-122 does not suppress T-tropic HIV infection and is inactive in calcium flux assay[1].
In Vivo
MSX-122 (10 mg/kg, i.p.) blocks inflammation induced by carrageenan and lung fibrosis induced by bleomycin in mice. MSX-122 (4 mg/kg, i.p., daily) blocks metastasis in an experimental animal model of breast cancer metastasis. Furthermore, MSX-122 (10 mg/kg i.p., daily) significantly decreases the numbers of hepatic micrometastases[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
