CCR4 Antagonist

C-021 dihydrochloride is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 dihydrochloride potently inhibits functional chemotaxis in human and mouse with IC₅₀s of 140 nM and 39 nM, respectively. C-021 dihydrochloride effectively prevents human CCL22-derived [³⁵S]GTPγS from binding to the receptor with an IC₅₀ of 18 nM.

GSK-2239633 is an indazole arylsulfonamide-based CCR4 antagonist. GSK-2239633 is applicable to research related to asthma.

ST45177901 is a CC chemokine receptor 4 (CCR4) antagonist. The combination of ST45177901 and Sorafenib (HY-10201) effectively inhibits the chemotaxis of Treg cells via the CCL22/CCL17-CCR4 signaling pathway, thereby significantly suppressing the growth and metastasis of tumor cells. ST45177901 is applicable to liver cancer research.

Tivumecirnon (FLX475) is an orally active, selective CCR4 antagonist. Tivumecirnon blocks the binding of CCR4 to its ligands, CCL17 and CCL22, thereby reducing Treg infiltration into the tumor microenvironment. Tivumecirnon has antitumor activity.

CCR4 antagonist 4 (compound 22) is a selective and potent antagonist of the CC chemokine receptor-4 (CCR4), with an IC₅₀ of 0.02 μM. CCR4 antagonist 4 also blocks MDC-mediated chemotaxis (IC₅₀: 0.007 μM) and Ca²⁺ mobilization (IC₅₀: 0.003 μM). CCR4 antagonist 4 can be used for allergic inflammation research.

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [¹²⁵I]-TARC to human CCR4 with a pIC₅₀ of 7.96.

CCR4-351 is an orally active, potent and selective CCR4 antagonist. CCR4-351, featuring a novel piperidinyl-azetidine motif, has IC₅₀s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 has antitumor activity.

CCR4-351 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4-351 hydrochloride, featuring a novel piperidinyl-azetidine motif, has IC₅₀s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4-351 hydrochloride has antitumor activity.

CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC₅₀ value of 1.7 μM for [¹²⁵I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM).