cxcr4

Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent CXCR4 antagonist with anti-angiogenic properties, potentially valuable in treating choroid neovascularization.

NUCC-390, a novel small-molecule CXCR4 receptor agonist, selectively induces CXCR4 receptor internalization while acting antagonistically to AMD3100. This compound facilitates nerve functional recovery following neurodegeneration in vivo.

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.

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

MSX-127 elicites positive response in peptide CXCR4.

ATI-2341 acetate is an effective allosteric agonist of CXCR4, it activates Gα1 instead of Gα13. ATI-2341 acetate activates inhibitory heterotrimeric G protein (GI) to promote the inhibition of cAMP production and induce calcium mobilization.

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

Motixafortide (BKT140 4-fluorobenzoyl) is a CXCR4 antagonist with an IC50 of 1 nM.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Ly2510924 acetate is an potent and selective CXCR4 antagonist. It prevents the binding of SDF-1 to CXCR4 with an IC50 of 0.079 nM.

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

WZ811 is a novel and effective small molecular CXCR4 antagonist (EC50: 0.3 nM).

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

Baohuoside I (Icariside-II) is a component of Epimedium koreanum, exhibits anti-inflammatory activity and anti-osteoporosis activities.

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

MSX-130 is CXCR4 Antagonist.

ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4), is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

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

Mogamulizumab (KW-0761) is a monoclonal antibody targeting T cell CC chemokine receptor 4. It exhibits anticancer activity by eliminating tumor cells through antibody-dependent cytotoxicity (ADCC) and can be used in the study of cancer, adult T-cell leukemia/lymphoma (ATLL), and cutaneous T-cell lymphoma (CTCL).

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.)

FC131 TFA (606968-52-9 free base) (FC131 TFA) is an antagonist of CXCR4 that inhibits the binding of [125I] -sdf-1 to CXCR4(IC50 : 4.5 nM ), and has anti-hiv activity.

ALX 40-4C acetate is a CXCR4 inhibitor of the chemokine receptor (Ki = 1 μM) and suppresses the replication of X4 strains of HIV-1. ALX 40-4C acetate is an antagonist of the APJ receptor (IC50 = 2.9 μM).

Balixafortide (POL6326) is a potent, selective, and well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM, and also acts as a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. It demonstrates anti-cancer effects[1][2], blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM, and is 1000-fold more selective for CXCR4 than a large panel of receptors, including CXCR7.