CCR7 Antagonist

CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a K_d of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC₅₀ of 7.3 μM.

Cosalane (NSC 658586) is a CCR7 (IC₅₀ = 2.43 μM) and CXCR2 antagonist (IC₅₀ = 0.66 μM). Cosalane is an inhibitor of HIV replication with a wide range of activity against HIV-1 isolates, HIV-2, Rauscher murine leukemia virus, HSV-1, HSV-2 and human cytomegalovirus. Cosalane inhibits both attachment of gp120 to CD4. Cosalane inhibits human and murine CCR7 in response to both CCL19 and CCL21 agonists. Cosalane can be studied in research for HIV or attenuating acute graft-versus-host disease (aGVHD) in allogeneic hematopoietic stem cell transplantation (HSCT).

CXCR2 antagonist 10 (Compound 10b) is a CCR2 antagonist with an IC₅₀ of 0.48 μM. CXCR2 antagonist 10 also exhibits antagonistic activity against CXCR2/CCR7, with IC₅₀ values of 4.18 μM and 2.07 μM, respectively. CXCR2 antagonist 10 is applicable for cancer research.

SLW131 is a CCR7 antagonist with a K_i value of 9.85 nM. SLW131 inhibits CCL19-induced Go protein activation with an IC₅₀ of 29.4 μM, and suppresses β-arrestin2 recruitment with an IC₅₀ of 6.0 μM. SLW131 serves as a probe for investigating the biological functions of CCR7 in cells. SLW131 is applicable to research related to rheumatoid arthritis.