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Isoform-selective Products

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CXCR Products

All (33)
CXCR Inhibitors (3)
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CXCR Antagonists (21)
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New CXCR Products

Catalog No.	Product Name	Information	Product Use Citations
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, 2024, 187(5):1223-1237.e16 Cell, 2024, 187(5):1223-1237.e16 Stem Cell Res Ther, 2024, 15(1):167
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.	Cell Rep, 2024, 43(2):113751 Biomed Pharmacother, 2024, 180:117526 Cytojournal, 2024, 21:28
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.	Sci Signal, 2024, 17(828):eabl3758 Cell Discov, 2023, 9(1):104 Cell Discov, 2023, 9(1):104
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).	Nat Commun, 2024, 15(1):7184 Redox Biol, 2024, 76:103323 J Immunother Cancer, 2024, 12(4)e008760
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.	Nat Commun, 2023, 14(1):5534 Nat Commun, 2023, 14(1):5534 J Gastroenterol, 2022, 10.1007/s00535-022-01928-x
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.	iScience, 2024, 27(8):110562 Mol Ther Oncol, 2024, 32(1):200777 Int J Mol Sci, 2024, 25(21)11592
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.	Inflammation, 2024, Cell Rep, 2023, 42(6):112566 Gut Microbes, 2022, 14(1):2096989
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.	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.	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.	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
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).
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.
E4650^New	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^New	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.
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.
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).	Nat Commun, 2024, 15(1):7184 Redox Biol, 2024, 76:103323 J Immunother Cancer, 2024, 12(4)e008760
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.	Cell Metab, 2024, 36(5):984-999.e8 Nat Commun, 2023, 14(1):4677
S3951	Tannic acid	Tannic acid (Gallotannic acid), a polyphenolic compound, is a CXCL12/CXCR4 inhibitor with antiangiogenic, anti-inflammatory and antitumor activity.
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.
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.
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.
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, 2024, 187(5):1223-1237.e16 Cell, 2024, 187(5):1223-1237.e16 Stem Cell Res Ther, 2024, 15(1):167
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.	Cell Rep, 2024, 43(2):113751 Biomed Pharmacother, 2024, 180:117526 Cytojournal, 2024, 21:28
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.	Sci Signal, 2024, 17(828):eabl3758 Cell Discov, 2023, 9(1):104 Cell Discov, 2023, 9(1):104
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.	Nat Commun, 2023, 14(1):5534 Nat Commun, 2023, 14(1):5534 J Gastroenterol, 2022, 10.1007/s00535-022-01928-x
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.	iScience, 2024, 27(8):110562 Mol Ther Oncol, 2024, 32(1):200777 Int J Mol Sci, 2024, 25(21)11592
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.	Inflammation, 2024, Cell Rep, 2023, 42(6):112566 Gut Microbes, 2022, 14(1):2096989
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.	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.	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).
E4650^New	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^New	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.
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).	Cell Discov, 2023, 9(1):104 Cell Discov, 2023, 9(1):104
E4650^New	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.
S0438^New	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.

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