CXCR

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Isoform-specific Inhibitors

Catalog No. Information Product Use Citations Product Validations
S8309New

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.

S3013

Plerixafor 8HCl (AMD3100 8HCl)

Plerixafor 8HCl (AMD3100 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.

S8030

Plerixafor (AMD3100)

Plerixafor (AMD3100) 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.

S2912

WZ811

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

S2879New

AMD3465

AMD3465 is a monomacrocyclic CXCR4 antagonist with IC50 of 0.75 nM.

S7651

SB225002

SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

Catalog No. Information Product Use Citations Product Validations
S3013

Plerixafor 8HCl (AMD3100 8HCl)

Plerixafor 8HCl (AMD3100 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.

2015, 10.1172/JCI80883

2014, 123(21):3296-304

2015, 10.15252/emmm.201404698

S8030

Plerixafor (AMD3100)

Plerixafor (AMD3100) 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.

2015, 125(8):3226-40

2014, 123(21):3296-304

2015, 10.15252/emmm.201404698

S2912

WZ811

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

2017, 40(1):47-62

2016, 8(9):3812-3821

S2879New

AMD3465

AMD3465 is a monomacrocyclic CXCR4 antagonist with IC50 of 0.75 nM.

S7651

SB225002

SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.

2016, 10.1177/1744806916646381

2016, 789:1-8

Catalog No. Information Product Use Citations Product Validations
S8309New

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.