CXCR4 Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S3951 Tannic acid

Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.

Selective
S8505 LY2510924

LY2510924 is a potent and selective CXCR4 antagonist that specifically blocks SDF-1 binding to CXCR4 with IC50 value of 0.079 nmol/L and inhibits SDF-1-induced GTP binding with Kb value of 0.38 nmol/L.

Selective CXCR4, IC50: 0.079 nM
S2912 WZ811

WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.

Selective CXCR4, EC50: 0.3 nM
S9665 Motixafortide (BL-8040)

Motixafortide (BL-8040, BKT140, TF 14016, 4-fluorobenzoyl, 4F-benzoyl-TN14003, T140) is an antagonist of CXCR4 with IC50 of ~1 nM. BL-8040 induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Selective CXCR4, IC50: 1 nM
S6617 MSX-122

MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).

Selective CXCR4, IC50: ~10 nM
S8030 Plerixafor (AMD3100)

Plerixafor (AMD3100, JM 3100, SID791) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor inhibits human immunodeficiency virus (HIV) replication.

Selective CXCR4, IC50: 44 nM
S3013 Plerixafor (AMD3100) 8HCl

Plerixafor (AMD3100, JM 3100) 8HCl is the hydrochloride of Plerixafor, a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively. Plerixafor can be used as an anti-HIV agent.

Selective CXCR4, IC50: 44 nM
S8309 ATI-2341

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.

Selective CXCR4, EC50: 194 nM
S8813 LIT-927

LIT-927 is a novel neutraligand of CXCL12 with Ki value of 267 nM for inhibition of Texas red-labeled CXCL12 (CXCL12-TR) binding. It shows high selectivity toward CXCL12 vs other chemokines also involved in asthma.

Selective
S9725 Balixafortide (POL6326)

Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist.

Selective
S2879 AMD3465 hexahydrobromide

AMD3465 is a monomacrocyclic CXCR4 antagonist.

Selective