CXCR

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CXCR Signaling Pathway Map

CXCR Signaling Pathways

CXCR Products

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  • CXCR Antagonists (17)
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  • 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.
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.
Cell Rep, 2022, 38(10):110490
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).
Cell Rep, 2022, 38(10):110490
Cell Death Discov, 2022, 8(1):235
J Exp Clin Cancer Res, 2021, 40(1):87
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.
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.
J Genet Genomics, 2022, S1673-8527(22)00125-4
Nat Commun, 2021, 12(1):652
Cell Rep, 2020, 33(1):108221
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.
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x
Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
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
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.
Gut Microbes, 2022, 14(1):2073785
Theranostics, 2022, 12(5):2063-2079
Oncogene, 2022, 10.1038/s41388-021-01920-4
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.
ACS Nano, 2022, 10.1021/acsnano.1c07492
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x
Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540
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.
J Biomed Mater Res B Appl Biomater, 2022, 10.1002/jbm.b.35021
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.
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.
Cell Rep, 2022, 38(10):110490
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).
Cell Rep, 2022, 38(10):110490
Cell Death Discov, 2022, 8(1):235
J Exp Clin Cancer Res, 2021, 40(1):87
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.
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.
J Genet Genomics, 2022, S1673-8527(22)00125-4
Nat Commun, 2021, 12(1):652
Cell Rep, 2020, 33(1):108221
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.
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x
Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540
Nat Cell Biol, 2021, 10.1038/s41556-021-00766-y
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
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.
Gut Microbes, 2022, 14(1):2073785
Theranostics, 2022, 12(5):2063-2079
Oncogene, 2022, 10.1038/s41388-021-01920-4
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.
ACS Nano, 2022, 10.1021/acsnano.1c07492
Acta Pharmacol Sin, 2022, 10.1038/s41401-022-00901-x
Kaohsiung J Med Sci, 2022, 10.1002/kjm2.12540
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.
J Biomed Mater Res B Appl Biomater, 2022, 10.1002/jbm.b.35021
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.
Tags: CXCR inhibitor|CXCR agonist|CXCR activator|CXCR inducer|CXCR antagonist|CXCR signaling pathway|CXCR assay kit