CXCR

Inhibitory Selectivity
Catalog No.Inhibitor Name CXCR1CXCR2CXCR4Other
A10913Plerixafor 8HCl
**
CXCL12-mediated chemotaxis
A13074Plerixafor
**
CXCL12-mediated chemotaxis
A12588WZ811
****
A14209SB225002
***
A16351ATI-2341
*
A14997AMD-070 HCl
***
A15234SCH 563705
****
***
A14209SB225002
***
A11555SCH-527123 (Navarixin)
**
***
A12383Reparixin
****
**
CXCL8
A12596MSX-122
***
A11315AMD 070
***

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.



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Catalog No. Product Name Application Product Information
A10913 SALE

Plerixafor 8HCl (DB06809)

CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.
A15941

AZD-5069

CXCR2 antagonist
AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD.
A15439

UNBS5162

CXCL chemokines antagonist
UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.
A14997

AMD-070 HCl

CXCR4 antagonist
AMD-070 hydrochloride is a potent and selective antagonist of CXCR4 with an IC50 value of 13 nM in a CXCR4 125I-SDF inhibition binding assay, inhibit the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs.
A15234

SCH 563705

CXCR2/CXCR1 antagonist
SCH 563705 is a potent dual CXCR2(IC50= 1.3 nM)/CXCR1(IC50= 7.3 nM) antagonist.
A15219

Reparixin L-lysine salt

CXCL8 receptor inhibitor
Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
A14209 SALE

SB225002

CXCR2 antagonist
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.
A14195

SB265610

CXCR2 antagonist
SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.
A11555

SCH-527123 (Navarixin)

CXCR1/CXCR2 antagonist
SCH527123 is a potent and selective antagonist of the human CXCR1 and CXCR2 receptors with IC50 of 42 nM and 3 nM, respectively.
A13074 SALE

AMD3100 (Plerixafor)

CXCR4 antagonist
Plerixafor is an immunostimulant used to multiply hematopoietic stem cells and it is a chemokine receptor-4 antagonist for mobilization of hematopoietic stem cells for transplantation.
A12383 SALE

Reparixin

CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
A11577

SRT3190

SIRT1 activator
SRT3190 is a potent CXCR2 ligand.
A12596 SALE

MSX-122

CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration.
A12588

WZ811

CXCR4 antagonist
WZ811 is a C-X-C chemokine receptor type 4 (CXCR4) antagonist (EC50 = 0.3 nM). Inhibits CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cAMP in vitro (EC50 = 1.2 nM).
A11097

SRT3109

CXCR2 ligand
SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
A11953 SALE

AMD 3465 Hexahydrobromide

CXCR4 antagonist
AMD 3465 is a potent, selective CXCR4 antagonist.
A11315 SALE

AMD 070

CXCR4 antagonist
AMD 070 is a CXCR4 chemokine receptor antagonist.
A16351

ATI-2341

CXCR4 agonist
ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4) (EC50 = 194 nM, is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.

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