CXCR4 Inhibitor

Baohuoside I, a flavonoid isolated from Epimedium koreanum Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 expression, induces apoptosis and shows anti-tumor activity.

LY2510924 is a potent and selective CXCR4 antagonist that blocks SDF-1 binding to CXCR4 with an IC₅₀ of 0.079 nM.

KY1051 is a human monoclonal antibody targeting CXCR4/CD184. KY1051 can be used for research related to tumor immunology.

ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a K_i of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC₅₀ of 2.9 μM.

CCX662 is a selective CXCR7 inhibitor with human IC₅₀ values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC₅₀ of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4⁺/CXCR7⁺ cells. CCX662 can be used for the research of glioblastoma multiforme.

CXCR4-IN-3 (compound XVI) is an orally active and potent inhibitor targeting the inflammation-related receptor CXCR4, with an IC₅₀ of 3.2 nM. CXCR4-IN-3 exhibits potent antichemotactic activity, at 79.19±2.33% inhibition. CXCR4-IN-3 shows anti-inflammatory activity. CXCR4-IN-3 can be used for IBD (inflammatory bowel disease) research.

CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC₅₀ of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research.

Hit 14 is an inhibitor for C-X-C chemokine receptor type 4 (CXCR4) with IC₅₀ of 254 nM. Hit 14 inhibits the migration and invasion of cell MDA-MB-231. Hit 14 inhibits the Akt phosphorylation, exhibits anti-inflammatory activity, and ameliorateds the ear swelling and damage in mouse models.

ALX 40-4C is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a K_i of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC₅₀ of 2.9 μM.

CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC₅₀ of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus.

Cyclazosin is an α₁D-adrenergic receptor antagonist and a partial agonist of CXCR4/ACKR3. The pKi values of Cyclazosin for cloned human α₁D, α₁B and α₁A adrenergic receptors are 9.28, 9.23 and 8.18, respectively. Cyclazosin induces β-arrestin recruitment in CXCR4 and ACKR3 with EC50 values of 16 μM and 10 μM, respectively, stimulates ERK1/2 phosphorylation, and induces receptor internalization. Cyclazosin potently inhibits CXCL12-induced chemotaxis of primary human aortic vascular smooth muscle cells. Cyclazosin alters MDMA-induced thermoregulatory responses in mice, converting monophasic hyperthermia to a biphasic pattern without affecting resting core body temperature. Cyclazosin can be used for diseases related to tumor metastasis, MDMA-induced hyperthermia and vasoconstriction.

PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies.

ALX-0651 is a biparatopic humanized monoclonal antibody inhibitor targeting CXCR4. ALX-0651 inhibits hematopoietic stem cell trafficking, tumor progression and metastasis. ALX-0651 can be used for non-Hodgkin’s lymphoma and multiple myeloma research.