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

CXCR4 Antagonist

CXCR4 Antagonists (39):

Cat. No. Product Name Effect Purity
  • HY-P4111
    Peptide R
    		Antagonist
    Peptide R, a cyclic peptide, is a specific CXCR4 antagonist. Peptide R shows outstanding capacities to profoundly remodel the tumor stroma. Peptide R has the potential for tumor research.
  • 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. Mavorixafor can be used for the study of WHIM syndrome.
  • HY-103010
    MSX-130
    		Antagonist 98.00%
    MSX-130 is a CXCR4 antagonist. MSX-130 inhibits cancer metastasis.
  • HY-122058A
    KRH-3955 hydrochloride
    		Antagonist
    KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
  • HY-P1104
    FC131
    		Antagonist
    FC131 is a potent CXCR4 antagonist. FC131 inhibits [125I]-SDF-1 binding to CXCR4 with an IC50 of 4.5 nM. FC131 has anti-HIV activity.
  • HY-P1682
    Balixafortide
    		Antagonist
    Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.
  • HY-147808
    CXCR4 antagonist 7
    		Antagonist
    CXCR4 antagonist 7 (Compound PARA-B) is a CXCR4 antagonist with the IC50 of 9.3 nM. CXCR4 antagonist 7 can be used for the research of HIV infection, inflammatory diseases, cancer, and WHIM syndrome.
  • HY-P1103A
    CTCE-9908 TFA
    		Antagonist
    CTCE-9908 TFA is a potent and selective CXCR4 antagonist. CTCE-9908 TFA induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
  • HY-146372
    CXCR4 antagonist 5
    		Antagonist
    CXCR4 antagonist 5 (compound 23) is a highly potent CXCR4 antagonist with an IC50 value of 8.8 nM. CXCR4 antagonist 5 can inhibit CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and inhibits CXCR4/CXLC12-mediated chemotaxis. CXCR4 antagonist 5 has good physicochemical properties and in vitro safety profiles, inhibiting CYP isozymes and hERG marginally or moderately.
  • HY-147979
    CXCR4 antagonist 9
    		Antagonist
    CXCR4 antagonist 9 (Compound 2) is a CXCR4 antagonist with an IC50 of 15 nM. CXCR4 antagonist 9 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 1.3 nM.
  • HY-144285
    CXCR4 antagonist 4
    		Antagonist
    CXCR4 antagonist 4 is a potent, orally active CXCR4 antagonist (IC50=24 nM) with diminished CYP 2D6 activity, improved PAMPA permeability, potent inhibition of human immunodeficiency virus entry (IC50=7 nM).
  • HY-115493
    TIQ-15
    		Antagonist
    TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM.
  • HY-147978
    CXCR4 antagonist 8
    		Antagonist
    CXCR4 antagonist 8 (Compound 3) is a CXCR4 antagonist with an IC50 of 57 nM. CXCR4 antagonist 8 inhibits CXCL12 induced cytosolic calcium increase with an IC50 of 0.24 nM. CXCR4 antagonist 8 inhibits CXLC12/CXCR4 mediated cell migration.
  • HY-136437
    CXCR4 antagonist 1
    		Antagonist
    CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity.
  • HY-146413
    HF50731
    		Antagonist
    HF50731 (compound 21) is a potent CXCR4 antagonist. HF50731 shows strong CXCR4 binding affinity, with IC50 of 19.8 nM. HF50731 effectively inhibits calcium mobilization, cell migration, and HIV-1 infection via CXCR4 coreceptor, with IC50 values of 119.2 nM, 621.4 nM and 1.5 μM.
  • HY-129094
    ICT5040
    		Antagonist
    ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells.
  • HY-P10429
    RCP168
    		Antagonist
    RCP168 is a highly selective and affinity CXCR4 receptor antagonist (IC50=5 nM). RCP168 has a stronger ability than natural chemical factors to inhibit the entry of HIV-1 (human immunodeficiency virus type 1) into host cells via CXCR4 receptors. RCP168 inhibits HIV-1 infection by blocking viral binding sites or inducing receptor internalization. RCP168 can be used to analyze the interaction between CXCR4 receptor and other chemical factor receptors.
  • HY-146401
    CXCR4 antagonist 6
    		Antagonist
    CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice.
  • HY-123819
    KRH-1636
    		Antagonist
    KRH-1636 is a CXC chemokine receptor (CXCR) 4 antagonist. KRH-1636 can be used in HIV-1 research.