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. |
-
Cell Mol Life Sci, 2025, 82(1):280
-
iScience, 2025, 28(1):111564
-
FEBS J, 2025, NONE
|
|
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.
|
-
Adv Sci (Weinh), 2025, 12(8):e2411711
-
Theranostics, 2025, 15(7):2852-2869
-
Cancer Immunol Res, 2025, 10.1158/2326-6066.CIR-24-1194
|
|
S3013 |
Plerixafor (AMD3100) 8HCl
|
Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 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. |
-
Angiogenesis, 2025, 28(3):26
-
Sci Signal, 2024, 17(828):eabl3758
-
iScience, 2024, 27(10):110862
|
|
S2912 |
WZ811
|
WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM. |
-
Front Immunol, 2024, 15:1389411
-
Neural Regen Res, 2024, 10.4103/NRR.NRR-D-24-00081
-
Cells, 2024, 13(5)408
|
|
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). |
-
Immunity, 2025, S1074-7613(25)00139-6
-
Nat Commun, 2025, 16(1):4128
-
Biomed Pharmacother, 2025, 188:118203
|
|
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. |
-
Cell Mol Life Sci, 2025, 82(1):280
-
Nat Commun, 2024, 15(1):10413
-
Nat Commun, 2023, 14(1):5534
|
|
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. |
-
Biomolecules, 2025, 15(5)645
-
iScience, 2024, 27(8):110562
-
Mol Ther Oncol, 2024, 32(1):200777
|
|
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. |
-
Front Immunol, 2025, 16:1552993
-
Inflammation, 2024,
-
Cell Rep, 2023, 42(6):112566
|
|
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). |
-
Cell Discov, 2023, 9(1):104
-
Cell Discov, 2023, 9(1):104
|
|
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. |
-
Front Physiol, 2024, 15:1349119
-
Nat Commun, 2023, 14(1):2207
|
|
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. |
-
Biomed Pharmacother, 2025, 188:118203
-
Biomolecules, 2025, 15(5)645
-
Cell Rep, 2022, 38(10):110490
|
|
S2879 |
AMD3465 hexahydrobromide
|
AMD3465 is a monomacrocyclic CXCR4 antagonist. |
-
Front Oncol, 2021, 11:708915
|
|
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. |
-
Nat Commun, 2025, 16(1):3905
-
Sci Rep, 2025, 15(1):20778
-
Front Immunol, 2022, 13:923492
|
|
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. |
-
Biomolecules, 2025, 15(5)645
-
Cell Metab, 2024, 36(5):984-999.e8
-
Nat Commun, 2023, 14(1):4677
|
|
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. |
-
Redox Biol, 2024, 76:103323
-
Theranostics, 2019, 9(18):5332-5346
|
|
S6617 |
MSX-122
|
MSX-122 (Q-122) is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM). |
-
Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.007
|
|
F1523New |
Anti-CXCL12/SDF-1 Mouse Antibody [N2D21]
|
SDF1,SDF-1,SDF1/CXCL12,SDF-1/CXCL12 |
|
|
E1318 |
Mavorixafor
|
Mavorixafor (AMD-070) is a potent, selective CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. |
|
|
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). |
|
|
E7614New |
NBI-74330
|
NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively. |
|
|
A2868 |
Anti-CXCL10 / IP-10 (NI-0801)
|
Anti-CXCL10 / IP-10 (NI-0801) is a fully human monoclonal antibody against chemokine (C-X-C motif) ligand 10 (CXCL10). It has the potential to treat primary biliary cholangitis. MW: 146.08. |
|
|
E4650New |
Ladarixin
|
Ladarixin(DF 2156A free base) is a small molecule, orally available, allosteric and non-competitive antagonist of dual CXCR1 and CXCR2. It is able to reduce the acute and chronic neutrophilic influx, and can be used in research of Asthma, Idiopathic Pulmonary Fibrosis, Influenza-A infection and COPD, cutaneous and uveal melanoma conditions. |
|
|
A2670 |
Anti-CXCL8 / IL-8 (HuMax-IL8)
|
Anti-CXCL8 / IL-8 (HuMax-IL8) is a monoclonal antibody targeting CXCL8. It has strong antitumor effect. MW :144.94 KD. |
|
|
A2706 |
Anti-CXCR3 / GPR9 / CD183
|
Anti-CXCR3 / GPR9 / CD183 is a monoclonal antibody binds to Chemokine (C-X-C motif) receptor 3 (CXCR3, also known as G protein-coupled receptor 9 (GPR9)) . It has the potentially to be used in the treatment of diabetes mellitus type I (T1D). MW: 146.38 KD. |
|
|
A2523 |
Ulocuplumab (Anti-CXCR4 / CD184)
|
Ulocuplumab (Anti-CXCR4 / CD184) is a fully human IgG4 antibody, targeting CXCR4. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models. MW: 144.84 KD. |
|
|
A2524 |
Anti-CXCL8 / IL-8
|
Anti-CXCL8 / IL-8 (ABX-IL8) is a antibody targeting CXCL8. MW: 145.5 KD. |
|
|
A2525 |
Eldelumab (Anti-CXCL10 / IP-10)
|
Eldelumab (Anti-CXCL10 / IP-10) is a humanised monoclonal antibody (IgG1 type) targeting CXCL10. Eldelumab selectively binds to CXCL10 and blocks CXCL10-induced calcium flux and cell migration. Eldelumab can be used in studies of autoimmune and auto-inflammatory diseases such as rheumatoid arthritis, ulcerative colitis and crohn's disease. MW: 145.5 KD. |
|
|
S3951 |
Tannic acid
|
Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity. |
|
|
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. |
|
|
A2721 |
Anti-CXCL4 / PF4
|
Anti-CXCL4 / PF4 is a monoclonal antibody against anti-CXC chemokine ligand 4 (CXCL4, also called PF4). MW: 144.86 KD. |
|
|
S0438 |
TAK-779
|
TAK-779(Takeda 779), a nonpeptide compound, is a potent antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5. It also exhibits highly potent and selective inhibition of R5 HIV-1 replication with EC50 and EC90 of 1.2 and 5.7 nM, respectively. It also suppresses the development of the cytokine storm in the murine model of the SARS-CoV-2-related acute respiratory distress syndrome. |
|
|
S9516 |
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. |
-
Biomed Pharmacother, 2025, 188:118203
|
|
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. |
|
|
E5984New |
ML339
|
ML339 is a potent and selective antagonist of CXCR6. ML339 antagonizes CXCL16-induced β-arrestin recruitment and cAMP signaling through the human CXCR6 receptor with IC50 values of 0.3 and 1.4 μM, respectively. ML339 shows no inhibitory activity against CXCR5, CXCR4, and CCR6. ML339 can be used as a potential agent for prostate cancer research. |
|
|
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. |
- Cell Mol Life Sci, 2025, 82(1):280
- iScience, 2025, 28(1):111564
- FEBS J, 2025, NONE
|
|
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.
|
- Adv Sci (Weinh), 2025, 12(8):e2411711
- Theranostics, 2025, 15(7):2852-2869
- Cancer Immunol Res, 2025, 10.1158/2326-6066.CIR-24-1194
|
|
S3013 |
Plerixafor (AMD3100) 8HCl
|
Plerixafor (AMD3100, JM 3100,Plerixafor Octahydrochloride,AMD3100 octahydrochloride,SID791 octahydrochloride) 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. |
- Angiogenesis, 2025, 28(3):26
- Sci Signal, 2024, 17(828):eabl3758
- iScience, 2024, 27(10):110862
|
|
S2912 |
WZ811
|
WZ811 is a highly potent competitive CXCR4 antagonist with EC50 of 0.3 nM. |
- Front Immunol, 2024, 15:1389411
- Neural Regen Res, 2024, 10.4103/NRR.NRR-D-24-00081
- Cells, 2024, 13(5)408
|
|
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. |
- Cell Mol Life Sci, 2025, 82(1):280
- Nat Commun, 2024, 15(1):10413
- Nat Commun, 2023, 14(1):5534
|
|
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. |
- Biomolecules, 2025, 15(5)645
- iScience, 2024, 27(8):110562
- Mol Ther Oncol, 2024, 32(1):200777
|
|
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. |
- Front Immunol, 2025, 16:1552993
- Inflammation, 2024,
- Cell Rep, 2023, 42(6):112566
|
|
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. |
- Front Physiol, 2024, 15:1349119
- Nat Commun, 2023, 14(1):2207
|
|
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. |
- Biomed Pharmacother, 2025, 188:118203
- Biomolecules, 2025, 15(5)645
- Cell Rep, 2022, 38(10):110490
|
|
S2879 |
AMD3465 hexahydrobromide
|
AMD3465 is a monomacrocyclic CXCR4 antagonist. |
- Front Oncol, 2021, 11:708915
|
|
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. |
- Nat Commun, 2025, 16(1):3905
- Sci Rep, 2025, 15(1):20778
- Front Immunol, 2022, 13:923492
|
|
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. |
- Redox Biol, 2024, 76:103323
- Theranostics, 2019, 9(18):5332-5346
|
|
S6617 |
MSX-122
|
MSX-122 (Q-122) is a novel small molecule and partial CXCR4 antagonist (IC50~10 nM). |
- Cell Mol Gastroenterol Hepatol, 2023, 10.1016/j.jcmgh.2023.10.007
|
|
E1318 |
Mavorixafor
|
Mavorixafor (AMD-070) is a potent, selective CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding. |
|
|
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). |
|
|
E4650New |
Ladarixin
|
Ladarixin(DF 2156A free base) is a small molecule, orally available, allosteric and non-competitive antagonist of dual CXCR1 and CXCR2. It is able to reduce the acute and chronic neutrophilic influx, and can be used in research of Asthma, Idiopathic Pulmonary Fibrosis, Influenza-A infection and COPD, cutaneous and uveal melanoma conditions. |
|
|
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. |
|
|
S0438 |
TAK-779
|
TAK-779(Takeda 779), a nonpeptide compound, is a potent antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5. It also exhibits highly potent and selective inhibition of R5 HIV-1 replication with EC50 and EC90 of 1.2 and 5.7 nM, respectively. It also suppresses the development of the cytokine storm in the murine model of the SARS-CoV-2-related acute respiratory distress syndrome. |
|
|
S9516 |
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. |
- Biomed Pharmacother, 2025, 188:118203
|
|
S9725 |
Balixafortide (POL6326)
|
Balixafortide (POL6326) is an orally bioavailable peptidic CXC chemokine receptor 4 (CXCR4) antagonist. |
|
|
E5984New |
ML339
|
ML339 is a potent and selective antagonist of CXCR6. ML339 antagonizes CXCL16-induced β-arrestin recruitment and cAMP signaling through the human CXCR6 receptor with IC50 values of 0.3 and 1.4 μM, respectively. ML339 shows no inhibitory activity against CXCR5, CXCR4, and CCR6. ML339 can be used as a potential agent for prostate cancer research. |
|
|