| Cat.No. | Name | Information |
|---|---|---|
| M3887 | SB225002 | SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM and >150-fold selectivity over CXCR1 and four other 7-TMRs. |
| M5160 | Reparixin | Reparixin is a noncompetitive allosteric inhibitor of IL-8 (CXCL8) activation of CXCR1 and CXCR2 chemokine receptors with IC50 of 1 and 100 nM, respectively. |
| M1898 | Plerixafor (AMD3100) | Plerixafor (AMD3100) is a CXCR4 chemokine receptor antagonist. |
| M28646 | PS372424 hydrochloride | PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation. |
| M28291 | TIQ-15 | TIQ-15 is a potent CXCR4 antagonist with an IC50 value of 6 nM for CXCR4 Ca2+ flux. TIQ-15 inhibits CYP450 2D6 with an IC50 value of 0.32 μM. |
| M28275 | USL311 | USL311 is a potent and selective CXCR4 antagonist, with anti-tumor activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4. |
| M28022 | SX-517 | SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model. |
| M27731 | NUCC-390 | NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 induces internalization of CXCR4 receptors and acts in an opposite way of AMD3100. NUCC-390 promotes nerve recovery of function after neurodegeneration in vivo. |
| M25401 | ACT-777991 | ACT-777991 is a highly potent, insurmountable, and selective CXCR3 antagonist that showed dose-dependent efficacy and target engagement in a mouse model of acute lung inflammation. |
| M25301 | Eldelumab | Eldelumab (BMS-936557) is a humanised anti-CXCL10 (IP-10) monoclonal antibody (IgG1 type). 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. |
| M24904 | Quetmolimab | Quetmolimab is a humanized anti-CX3CL1 monoclonal antibody. However, CX3CL1 is a chemokine with a modulating effect on chemotaxis and adhesion. |
| M24637 | Ulocuplumab | Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. 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. |
| M21355 | Vimnerixin | AZD4721 (RIST4721) is a potent and orally active antagonist of the acidic CXC chemokine receptor 2 (CXCR2).AZD4721 has the potential to investigate inflammatory diseases. |
| M21323 | ACT-660602 | ACT-660602 is an oral chemokine receptor CXCR3 antagonist with an IC50 of 204 nM. It is being developed for use in autoimmune diseases. |
| M20649 | 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. |
| M20617 | 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. |
| M13944 | Reparixin L-lysine salt | Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation. |
| M13943 | 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. |
| M13942 | IT1t dihydrochloride | IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM. |
| M13941 | CXCR2-IN-2 | CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). |
| M13938 | ALX 40-4C Trifluoroacetate | ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki of 1 μM, and suppresses the replication of X4 strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagonist of the APJ receptor, with an IC50 of 2.9 μM. |
| M11027 | SRT3190 | SRT3190 is an antagonist of CXCR2 that can be used in chemokine-mediated disease studies. |
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