tcsc1003 WZ811

WZ811 is a potent CXCR4 antagonist, effectively inhibits TN14003 binding to CXCR4, with an EC₅₀ of 0.3 nM.

IC50 & Target: EC50: 0.3 nM (CXCR4)^[1]

In Vitro: WZ811 (Compound 32) is a potent CXCR4 antagonist, effectively inhibits TN14003 binding to CXCR4, with an EC₅₀ of 0.3 nM. WZ811 also suppresses CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cyclic adenosine monophophate (cAMP) levels (EC₅₀, 1.2 nM) and SDF-1 induced Matrigel invasion (EC₅₀, 5.2 nM)^[1]. WZ811 (1, 5, 10, 20, 40 μM) inhibits TF-1 and UT-7 cells proliferation in a dose dependent manner both after treatment for 24 h and 48 h. Moreover, WZ811 (5 μM) induces cell apoptosis and enhances the sensitivity of cells to docetaxel. In addition, WZ811 inhibits aggressiveness markers and induces apoptosis in chronic lymphocytic leukemia cells^[2].

In Vivo: WZ811 (40 mg/kg, p.o.) blocks the lymphocytic leukemia cells growth on mouse xenograft models, and inhibits CXCR4/PI3K/AKT signaling pathway in mouse xenograft model of lymphocytic leukemia^[2].