cxcr4 antagonist 2

CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a 16-1 expression.

Peptide R, a cyclic peptide and specific CXCR4 antagonist, exhibits remarkable abilities to significantly alter tumor stroma. Its potential in tumor research is noteworthy [1] [2].

CXCR4 antagonist 9 (Compound 2) is a potent CXCR4 antagonist with an IC50 of 15 nM and effectively inhibits the cytosolic calcium increase induced by CXCL12, exhibiting an IC50 of 1.3 nM [1].

Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM, and also acts as a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. It demonstrates anti-cancer effects[1][2], blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM, and is 1000-fold more selective for CXCR4 than a large panel of receptors, including CXCR7.

AMD-3451 free base is a dual CCR5 CXCR4 antagonist which may be useful in the treatment of a wide variety of R5, R5 X4, and X4 strains of human immunodeficiency virus type 1 (HIV-1) and HIV-2. AMD3451 is the first low-molecular-weight anti-HIV agent with selective HIV coreceptor, CCR5 and CXCR4, interaction.

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

CTCE-9908 TFA, a potent and selective CXCR4 antagonist, triggers mitotic catastrophe and cytotoxicity, and suppresses migration in ovarian cancer cells expressing CXCR4 [1] [2].