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CXCR C X C Chemokine Receptor

Inhibitors

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.
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.
M21310 ACT-1004-1239 ACT-1004-1239 is a potent, selective, orally administered CXCR7 antagonist with an IC50 value of 3.2 nM.
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.
M13947 UNBS5162 UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.
M13946 SCH 563705 SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
M13945 SCH 546738 SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
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).
M13940 CXCR2-IN-1 CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3.
M13939 Mavorixafor trihydrochloride Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM, 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.
M10230 LY2510924 LY2510924 is a potent and selective CXCR4 antagonist, which blocks SDF-1 binding to CXCR4 with IC50 of 0.079 nM.
M10215 Motixafortide (BL-8040) Motixafortide (BL-8040, BKT140) is a synthetic cyclic peptide consisting of 14 amino acids and is an antagonist of CXCR4 with an IC50 value of approximately 1 nM.Motixafortide (BL-8040) is an antagonist of CXCR4 with an IC50 value of approximately 1 nM.
M10141 ATI-2341 TFA ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4).
M9821 SX-682 SX-682 is a potent and selective CXCR1/2 allosteric inhibitor, it may be useful for castration-resistant prostate cancer.



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