2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
  4. CXCR
  5. CXCR4 Isoform
  6. CXCR4 Antagonist

CXCR4 Antagonist

CXCR4 Antagonists (38):

Cat. No. Product Name Effect Purity
  • HY-10046
    Plerixafor
    		Antagonist 99.67%
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM.
  • HY-50912
    Plerixafor octahydrochloride
    		Antagonist ≥98.0%
    Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC50 of 44 nM.
  • HY-P0171
    Motixafortide
    		Antagonist 99.88%
    Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.
  • HY-50101A
    Mavorixafor trihydrochloride
    		Antagonist 99.75%
    Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-50101C
    Mavorixafor hydrochloride
    		Antagonist
    Mavorixafor (AMD-070) hydrochloride is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. Mavorixafor hydrochloride also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 nM and 9 nM, respectively.
  • HY-101458A
    IT1t dihydrochloride
    		Antagonist 99.77%
    IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-P1682A
    Balixafortide TFA
    		Antagonist 99.78%
    Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-15478
    WZ811
    		Antagonist 99.79%
    WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
  • HY-P99272
    Ulocuplumab
    		Antagonist 99.90%
    Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models.
  • HY-19867A
    Burixafor hydrobromide
    		Antagonist ≥98.0%
    Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well anti-angiogenic drug that is of potential value in treating choroid neovascularization. Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction.
  • HY-15971
    AMD 3465 hexahydrobromide
    		Antagonist ≥98.0%
    AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-13696
    MSX-122
    		Antagonist 98.92%
    MSX-122 is an orally active partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC50 of ∼10 nM. MSX-122 has anti-inflammatory and anti-metastatic activity.
  • HY-P1104A
    FC131 TFA
    		Antagonist 99.89%
    FC131 TFA is a CXCR4 antagonist, inhibits [125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
  • HY-P1103
    CTCE-9908
    		Antagonist 99.69%
    CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
  • HY-114244
    USL311
    		Antagonist 99.97%
    USL311 is a potent and selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
  • HY-15971A
    AMD 3465
    		Antagonist 99.59%
    AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
  • HY-103009
    MSX-127
    		Antagonist 99.68%
    MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.
  • HY-101458
    IT1t
    		Antagonist
    IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.
  • HY-50101
    Mavorixafor
    		Antagonist
    Mavorixafor (AMD-070) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, respectively.
  • HY-103010
    MSX-130
    		Antagonist 98.00%
    MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.