CXCR

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

CXCR Products

Catalog No. Information Product Use Citations Product Validations
S8947

SX-682

SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity.

S3951

Tannic acid

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

S8640

Reparixin (Repertaxin)

Reparixin (Repertaxin, DF 1681Y) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 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.

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.

S2912

WZ811

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

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.

S6645

AZD5069

AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.

S9725New

Balixafortide (POL6326)

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

S8682New

AMG 487

AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.

S9665New

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.

S0292

MSX-127

MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist.

S0293

MSX-130

MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4).

S2879

AMD3465 hexahydrobromide

AMD3465 is a monomacrocyclic CXCR4 antagonist.

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.

S6620

Danirixin (GSK1325756)

Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

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.

S6617

MSX-122

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

S4785

Nicotinamide N-oxide

Nicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. Nicotinamide N-oxide is novel, potent, and selective antagonists of the CXCR2 receptor.

S8506

Navarixin (SCH-527123)

Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.

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.

S8869

UNBS5162

UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7).

Catalog No. Information Product Use Citations Product Validations
S8947

SX-682

SX-682 is an orally bioavailable small-molecule allosteric inhibitor of CXCR1 and CXCR2 that blocks tumor MDSC recruitment and enhances T cell activation and antitumor immunity.

S3951

Tannic acid

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

S8640

Reparixin (Repertaxin)

Reparixin (Repertaxin, DF 1681Y) is a potent and specific inhibitor of CXCR1 with IC50 of 1 nM. Reparixin (Repertaxin) inhibits PMN migration induced by CXCL8 (IC50 = 1 nM) and rodent PMN chemotaxis induced by CXCL1 and CXCL2. Repertaxin inhibits the response of human PMN to CXCL1, which interacts with CXCR2 (IC50 = 400 nM).

Catalog No. Information Product Use Citations Product Validations
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.

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.

S2912

WZ811

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

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.

S6645

AZD5069

AZD5069 is a novel antagonist of CXCR2, which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.

S9725New

Balixafortide (POL6326)

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

S8682New

AMG 487

AMG 487 is an orally active and selective CXC chemokine receptor 3 (CXCR3) antagonist that inhibits the binding of IP-10 (CXCL10) and ITAC (CXCL11) to CXCR3 with IC50 of 8.0 nM and 8.2 nM, respectively.

S9665New

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.

S0292

MSX-127

MSX-127 (NSC-23026) is a C-X-C chemokine receptor type 4 (CXCR4) receptor antagonist.

S0293

MSX-130

MSX-130 is an antagonist of C-X-C chemokine receptor type 4 (CXCR4).

S2879

AMD3465 hexahydrobromide

AMD3465 is a monomacrocyclic CXCR4 antagonist.

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.

S6620

Danirixin (GSK1325756)

Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

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.

S6617

MSX-122

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

S4785

Nicotinamide N-oxide

Nicotinamide N-oxide (Nicotinamide 1-oxide, 1-oxynicotinamide) is recognized as an in vivo metabolite of nicotinamide which is a precurser of nicotinamide-adenine dinucleotide (NAD+) in animals. Nicotinamide N-oxide is novel, potent, and selective antagonists of the CXCR2 receptor.

S8506

Navarixin (SCH-527123)

Navarixin (SCH-527123, MK-7123, PS-291822) is a potent, orally bioavailable CXCR2/CXCR1 antagonist with IC50 values of 2.6 nM and 36 nM, respectively.

Catalog No. Information Product Use Citations Product Validations
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.

Catalog No. Information Product Use Citations Product Validations
S8869

UNBS5162

UNBS5162 is a pan-antagonist of CXCL chemokine expression with in vitro cytotoxic activity (IC50 range of 0.5-5 µM) against a range of human cancer cell lines including glioblastoma (Hs683 and U373MG), colorectal (HCT-15 and LoVo), non-small-cell lung (A549) and breast (MCF-7).