CXCR4 Antagonist

CXCR4 Antagonists (39):

Cat. No.	Product Name	Effect	Purity

HY-10046

Plerixafor	Antagonist	99.90%
Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM.

HY-50912

Plerixafor octahydrochloride	Antagonist	99.09%
Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM.

HY-P0171

Motixafortide	Antagonist	99.88%
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC₅₀ vakue of ～1 nM.

HY-50101A

Mavorixafor trihydrochloride	Antagonist	99.75%
Mavorixafor trihydrochloride (AMD-070 trihydrochloride) 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 trihydrochloride can be used for the study of WHIM syndrome.

HY-P4111A

Peptide R TFA	Antagonist	98.34%
Peptide R (TFA) is a synthetic and specific CXCR4 antagonist. Peptide R (TFA) shows outstanding capacities to remodel the tumor stroma. Peptide R (TFA) can be used for solid tumor (glioblastoma, etc.) research.

HY-101458A

IT1t dihydrochloride	Antagonist	99.77%
IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC₅₀ of 2.1 nM.

HY-P99272

Ulocuplumab	Antagonist	99.90%
Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models.

HY-P1682A

Balixafortide TFA	Antagonist	99.78%
Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC₅₀ < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC₅₀s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects.

HY-15478

WZ811	Antagonist	99.80%
WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC₅₀=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC₅₀=5.2 nM).

HY-19867A

Burixafor hydrobromide	Antagonist	≥98.0%
Burixafor (TG-0054) hydrobromide is a selective, orally active CXCR4 antagonist that effectively blocks the interaction between CXCR4 and its ligand, stromal cell-derived factor SDF-1. Burixafor hydrobromide interferes with the SDF-1/CXCR4 signaling pathway, prompting the release of bone marrow stem cells into the peripheral circulation, exerting immunomodulatory and anti-inflammatory activities. Burixafor hydrobromide can be used in the study of cancer, Intraocular neovascular diseases (such as choroidal neovascularization), myocardial infarction and other diseases, with the potential to mobilize stem cells, improve cardiac function and reduce inflammatory responses.

HY-15971

AMD 3465 hexahydrobromide	Antagonist	≥98.0%
AMD 3465 hexahydrobromide (GENZ-644494 hexahydrobromide) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 to CXCR4, with IC₅₀s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC₅₀: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

HY-13696

MSX-122	Antagonist	98.92%
MSX-122 is an orally active partial antagonist of CXCR4, inhibiting CXCR4/CXCL12 actions, with an IC₅₀ of ∼10 nM. MSX-122 has anti-inflammatory and anti-metastatic activity.

HY-P1104A

FC131 TFA	Antagonist	99.89%
FC131 TFA is a CXCR4 antagonist, inhibits [¹²⁵I]-SDF-1 binding to CXCR4, with an IC₅₀ of 4.5 nM. Anti-HIV activity.

HY-P1103

CTCE-9908	Antagonist	99.47%
CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.

HY-15971A

AMD 3465	Antagonist	99.59%
AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12^AF647 to CXCR4, with IC₅₀s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC₅₀: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

HY-114244

USL311	Antagonist	99.97%
USL311 is a potent and selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.

HY-P10415

EPI-X4	Antagonist	99.21%
EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC₅₀ of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC₅₀ of 8.6 μM.

HY-103009

MSX-127	Antagonist	99.68%
MSX-127 is a CXCR4 antagonist. MSX-127 inhibits cancer metastasis.

HY-50101C

Mavorixafor hydrochloride	Antagonist	99.10%
Mavorixafor (AMD-070) hydrochloride is a potent, selective and orally available CXCR4 antagonist, with an IC₅₀ value of 13 nM against CXCR4 ¹²⁵I-SDF binding. Mavorixafor hydrochloride also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC₅₀ of 1 nM and 9 nM, respectively. Mavorixafor hydrochloride can be used for the study of WHIM syndrome.

HY-101458

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

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