cxcl12/cxcr4

IT1t dihydrochloride inhibits CXCL12/CXCR4 interaction with IC50 of 2.1 nM. IT1t dihydrochloride is an antagonist of CXCR4.

IT1t inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. is a potent CXCR4 antagonist.

AMD-070 hydrochloride is a CXCR4 antagonist, is useful for Anti HIV.

CXCR4 antagonist 7 (Compound PARA-B) is a potent CXCR4 inhibitor (IC50 = 9.3 nM) [1] applicable in research on HIV infection, inflammatory diseases, cancer, and WHIM syndrome.

Tannic acid (Gallotannic acid) is a novel hERG channel blocker.

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

Plerixafor octahydrochloride (JM3100 octahydrochloride) blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4, resulting in hematopoietic stem cell (HSC) release from bone marrow and HSC movement into the peripheral circulation. Plerixafor is a bicyclam with hematopoietic stem cell-mobilizing activity.

CXCR4 antagonist 6 (compound 46) is a highly potent small-molecule inhibitor of the chemokine receptor CXCR4 with an IC50 value of 79 nM, effectively suppressing CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, significantly inhibiting CXCL12/CXCR4-mediated cell migration, and demonstrating pronounced therapeutic efficacy in a mouse model of cancer metastasis, highlighting its value for cancer biology, metastasis research, and chemokine signaling studies.

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. USL311 inhibits CXCR4 activation and decreases proliferation and migration of CXCR4-expressing tumor cells, with anti-tumor activ

CXCR4 antagonist 10 is a small-molecule antagonist of the chemokine receptor CXCR4 that inhibits related signaling pathways and cell migration by blocking the binding of CXCR4 to its ligand, CXCL12 (SDF-1). In vitro studies have shown that CXCR4 antagonist 10 can interfere with tumor cell metastasis and immune cell chemotaxis, demonstrating potential value in antitumor and anti-inflammatory research.

Burixafor (also known as TG-0054) is an orally available inhibitor of the CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell mobilization activities. By binding to the CXCR4 chemokine receptor, Burixafor blocks the binding and subsequent activation of stromal cell-derived factor-1 (SDF-1 or CXCL12) with the CXCR4 receptor, potentially facilitating the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the bloodstream. Note: Elemental analysis shows that this compound is a salt containing 3 HBr and 3 water molecules.

MSX-122 is a novel small molecule and partial CXCR4 antagonist, with potent inhibition of CXCR4/CXCL12 actions(IC50 = 10 nM).

CXCR4 antagonist 8 (Compound 3) is a potent inhibitor of CXCR4, exhibiting an IC50 value of 57 nM in antagonism and effectively inhibiting CXCL12-induced cytosolic calcium increase with an IC50 of 0.24 nM. Additionally, Compound 3 is efficacious in inhibiting CXCL12/CXCR4-mediated cell migration [1].

CXCR4 antagonist 5 (compound 23), a potent CXCR4 antagonist, exhibits high inhibition efficacy against CXCR4 with an IC50 value of 8.8 nM. It effectively suppresses CXCL12-induced cytosolic calcium increase (IC50 = 0.02 nM) and hinders CXCR4/CXCL12-mediated chemotaxis. Moreover, Compound 23 demonstrates favorable physicochemical properties and in vitro safety profiles, exhibiting only marginal to moderate inhibition of CYP isozymes and hERG [1].

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].

AMD 3465 hexahydrobromide (GENZ-644494 (hexahydrobromide)) is a CXCR4 receptor antagonist with potential anticancer and anti-HIV activity.

Ulocuplumab (BMS-936564) is a fully human anti-CXCR4 IgG4 antibody.Ulocplumab exhibits antitumor activity in acute myeloid leukemia (AML), non-Hodgkin's lymphoma (NHL), and multiple myeloma transplantation models.Ulocplumab inhibits the migration of chronic lymphocytic leukemia (CLL) cells under CXCR4 activation, induces apoptosis, and inhibits the growth and migration of cancer cells. Ulocplumab inhibits CXCL12-mediated chronic lymphocytic leukemia (CLL) cell migration in response to CXCR4 activation and induces apoptosis.)

EPI-X4, an endogenous peptide fragment of human serum albumin (amino acids 408-423), serves as an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4). It effectively prevents calcium mobilization and receptor internalization triggered by chemokine (C-X-C motif) ligand 12 (CXCL12) in HEK293 cells with CXCR4 expression, at concentrations between 0.8 and 1,000 µM. Moreover, EPI-X4 hampers the CXCL12-driven migration of both Jurkat T cells and human CD34+ hematopoietic stem cells. In an acute allergic airway hypereosinophilia mouse model, EPI-X4 intrinsically decreases Cxcr4-dependent inflammatory cell infiltration in airways at a dose of 16 µmol/kg. Additionally, increased urinary EPI-X4 levels, inversely related to glomerular filtration rate (GFR), are observed in chronic kidney disease patients, indicating its potential biomarker role.

TC 14012, a peptidomimetic compound, acts as both an antagonist to the chemokine (C-X-C motif) receptor 4 (CXCR4; IC50 = 2.9 nM) and as an agonist for CXCR7, effectively recruiting β-arrestin in HEK293T cells that express CXCR7 (EC50 = 350 nM). Moreover, it demonstrates significant antiviral activity by reducing the cytopathic effects of HIV in MT-4 cells with an EC50 value of 0.4 nM and inhibiting HIV entry in vitro through a CXCR4-dependent pathway (IC50 = 19.3 nM). Additionally, TC 14012 suppresses chemokine (C-X-C motif) ligand 12 (CXCL12)-induced migration in MDA-MB-231 breast cancer and human umbilical vein endothelial cells (HUVECs) within the 10 to 1,000 nM concentration range. In a mouse model, administration of TC 14012 at 10 mg/kg significantly reduced infarct size following acute myocardial infarction induced by ligation of the left anterior descending (LAD) coronary artery.

Anti-CXCL12/SDF1a Antibody is a monoclonal antibody specifically targeting Stromal Cell-Derived Factor-1α (SDF-1α/CXCL12). The compound binds to the CXCL12 protein, blocking its interaction with the receptors CXCR4 and CXCR7, thereby inhibiting chemokine-mediated downstream signaling. In experimental research, this antibody is frequently utilized to block directional immune cell migration, suppress tumor cell invasion and metastasis, and attenuate pathological angiogenesis.

Anti-CXCR4/CD184 Antibody represents a highly specialized monoclonal antibody specifically engineered to target the human C-X-C chemokine receptor type 4 (CXCR4) with exceptional binding affinity. It effectively facilitates the measurable blockade of the CXCL12/CXCR4 signaling axis across various preclinical experimental models to evaluate the modulation of cellular chemotaxis, hematopoietic stem cell mobilization, and the inhibition of tumor metastasis during strictly monitored laboratory observation periods and functional cell migration assays.

Minecoside is a CXCR4/STAT3 inhibitor with anticancer and anti-inflammatory activity. Minecoside decreases CXCR4 expression and suppresses STAT3 activation, thereby inhibiting CXCL12-induced invasion. Minecoside is utilized in biomedical research investigating chemokine receptor signaling, STAT3-dependent transcriptional regulation, metastatic invasion mechanisms, and apoptotic pathway modulation in disease models.

EPI-X4 (hSA408–423 peptide), with an IC50 of 8.6 μM, serves as an antagonist for the C-X-C motif chemokine receptor 4 (CXCR4). It inhibits CXCL12-mediated signaling and reduces chemokine-driven migration and invasion of leukemia cells. Furthermore, it demonstrates anti-inflammatory effects in a mouse model and possesses antiviral properties against CXCR4-tropic HIV, maintaining the same IC50.