CXCR

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CXCR Signaling Pathway Map

CXCR Signaling Pathways

CXCR Products

  • All (25)
  • CXCR Inhibitors (3)
  • CXCR Antibodies (2)
  • CXCR Antagonists (18)
  • CXCR Agonists (1)
  • CXCR Modulators (1)
  • New CXCR Products
Catalog No. Product Name Information Product Use Citations Product Validations
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).
J Exp Clin Cancer Res, 2021, 40(1):87
JCI Insight, 2021, 6(18)e150862
Ecotoxicol Environ Saf, 2021, 208:111693
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.
A5207 CXCR3 Rabbit Recombinant mAb CXCR3 Rabbit Recombinant mAb detects endogenous level of total CXCR3.
A5226 CXCR7 Rabbit Recombinant mAb CXCR7 Rabbit Recombinant mAb detects endogenous level of total CXCR7.
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.
S2912 WZ811 WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.
Nat Commun, 2021, 12(1):652
Cell Rep, 2020, 33(1):108221
Cell Death Dis, 2019, 10(9):648
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.
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
Adv Sci (Weinh), 2021, e2100584
Mol Cancer, 2021, 20(1):166
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.
S6617 MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
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.
Theranostics, 2019, 9(18):5332-5346
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.
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.
Theranostics, 2021, 11(20):10074-10090
Cell Rep, 2021, 36(2):109386
Mol Cancer, 2021, 20(1):62
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.
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
Adv Sci (Weinh), 2021, e2100584
Mol Cancer, 2021, 20(1):166
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.
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.
S8682 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.
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.
S9516New SB 265610 SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site.
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.
S9725 Balixafortide (POL6326)

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

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).
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).
J Exp Clin Cancer Res, 2021, 40(1):87
JCI Insight, 2021, 6(18)e150862
Ecotoxicol Environ Saf, 2021, 208:111693
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.
A5207 CXCR3 Rabbit Recombinant mAb CXCR3 Rabbit Recombinant mAb detects endogenous level of total CXCR3.
A5226 CXCR7 Rabbit Recombinant mAb CXCR7 Rabbit Recombinant mAb detects endogenous level of total CXCR7.
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.
S2912 WZ811 WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM.
Nat Commun, 2021, 12(1):652
Cell Rep, 2020, 33(1):108221
Cell Death Dis, 2019, 10(9):648
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.
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
Adv Sci (Weinh), 2021, e2100584
Mol Cancer, 2021, 20(1):166
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.
S6617 MSX-122 MSX-122 is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM).
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.
Theranostics, 2019, 9(18):5332-5346
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.
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.
Theranostics, 2021, 11(20):10074-10090
Cell Rep, 2021, 36(2):109386
Mol Cancer, 2021, 20(1):62
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.
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
Adv Sci (Weinh), 2021, e2100584
Mol Cancer, 2021, 20(1):166
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.
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.
S8682 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.
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.
S9516New SB 265610 SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site.
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.
S9725 Balixafortide (POL6326)

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

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).
S9516New SB 265610 SB265610, a competitive antagonist at the human CXCR2 receptor, can displace [125I]-IL-8 and [125I]-GROα with pIC50 values of 8.41 and 8.47 respectively, preventing receptor activation by binding to a region distinct from the agonist binding site.