CXCR4 Antagonist

CXCR4-antagonist-11 is a CXCR4 antagonist with CXCR4 IC₅₀ values of 68.9 nM and 48.3 nM. CXCR4-antagonist-11 modulates CXCR4 receptor function. CXCR4-antagonist-11 demonstrates high permeability, selectivity against CYP 2D6, and a high hERG index. CXCR4-antagonist-11 shows improved oral exposure in mouse pharmacokinetic studies.

DV1 is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases.

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.

MEDI-3185 is a potent CXCR4 antagonist. MEDI-3185 binds CXCR4 via CDR3H and ECL2 β-strand/β-strand interaction, blocks SDF-1 access and displaces SDF-1. MEDI-3185 can be used for the research of hematologic tumors, ovarian tumors.

IS4 is a selective CXCR4 competitive antagonist, with an IC₅₀ of 0.65 nM in THP-1 cells and 38.75 nM in Jurkat cells. IS4 is stable in serum and non-cytotoxic. IS4 competitively binds to CXCR4 with CXCL12, thereby inhibiting CXCL12-induced intracellular Ca²⁺ release and cancer cell migration. IS4 can be used in the research on the prevention of metastasis of breast cancer, prostate cancer, leukemia, and other diseases.

CXCR4 antagonist 1 is a potent CXCR4 antagonist. CXCR4 antagonist 1 has anti-HIV activity.

Peptide R54 (Pep R54) is a CXCR4 antagonist. Peptide R54 inhibits CXCL12-dependent activation of pERK1/2 and pAKT. The combination of Peptide R54 and Nivolumab (HY-P9903) suppresses melanoma growth. Peptide R54 (acetate) is applicable to research related to melanoma and ovarian cancer.

BPRCX 714 is a CXCR4 (CXC chemokine receptor type 4) receptor antagonist. BPRCX 714 can be used for the study of hepatocellular carcinoma.

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.

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.

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.

KRH-1636 is a CXC chemokine receptor (CXCR) 4 antagonist. KRH-1636 can be used in HIV-1 research.