ccr4

CCR4 antagonist 3-1 is a less active chemokine receptor 4 (CCR4) antagonist that inhibits [125I]TARC (thymus and activation-regulated chemokine) with an IC50 value of 1.7 μM. CCR4 antagonist 3-1 inhibits the binding of radiolabeled [125I]TARC and macrophage-derived chemokine ( MDC) to CEM cell surface and inhibits TARC-mediated CEM cell migration in vitro with an IC50 value of 6.4 μM. CCR4 antagonist 3 inhibited the binding of radiolabeled [125I]TARC and macrophage-derived chemokine (MDC) to the CCR4 receptor on the surface of CEM cells and inhibited TARC-mediated migration of CEM cells in vitro with an IC50 value of 6.4 μM.

CCR4 antagonist 2 (Compound 31) is a novel, potent, orally bioavailable small molecule antagonist of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues. CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca2+ flux and [chemotaxis] CTX at 40 nM and 70 nM, respectively.

CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.

CCR4 antagonist 3 hydrochloride is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC 50 s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.

CCR4 Antagonist 4 (Compound 22) is a potent and selective antagonist of the CC chemokine receptor-4 (CCR4), displaying an IC50 value of 0.02 μM. It also inhibits MDC-mediated chemotaxis and Ca2+ mobilization, with IC50 values of 0.007 μM and 0.003 μM, respectively. This compound is utilized in research on allergic inflammation [1].

C-021 dihydrochloride is a potent CCR4 antagonist that effectively inhibits functional chemotaxis in humans and mice, with IC50 values of 140 nM and 39 nM, respectively.

K777 is a potent, orally active, and irreversible inhibitor of cysteine protease, functioning as a potent CYP3A4 inhibitor (IC50 = 60 nM) and a selective CCR4 antagonist, which inhibits chemotaxis. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypanosoma cruzi, and cathepsins B and L, targeting cathepsin-mediated cell entry and exhibiting broad-spectrum antiviral activity. It inhibits EBOV and SARS-CoV pseudovirus entry with IC50 values of 0.87 nM and 0.68 nM, respectively.

C 021 dihydrochloride is a potent CCR4 antagonist. C-021 (4-Quinazolinamine, 2-[1,4'-bipiperidin]-1'-yl-N-cycloheptyl-6,7-dimethoxy-) dihydrochloride potently inhibits functional chemotaxis in humans and mice with IC50s of 140 nM and 39 nM, respectively. It effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor (IC50: 18 nM).

AF 399 is a CCR4 antagonist. It reverses the tumor-promoting environment.

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

J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

AZD-1678, [3-(2-(2-(2-hydroxyethoxy)ethoxy)ethoxy)-2-methoxyphenyl]-(2-(4-((E)-2-(2-(thiophen-3-yl)vinyl)pyrrolidin-1-yl)methyl)benzyl)amine, is a potent CCR4 receptor antagonist.

ZK 756326 is a selective, non-peptide CCR8 chemokine receptor agonist (IC50: 1.8 μM, in human; 2.6 μM, in mouse). Displays no activity at CCR4 5 and CXCR3 4 and shows higher 28-fold selectivity over 26 other GPCRs (less selective at α2A and 5-HT receptors). Induces chemotaxis and inhibits Env-mediated (HIV) cell-cell fusion.

AZD2098 is a potent CC-chemokine receptor 4 (CCR4) inhibitor used for asthma research.

RPT193 is an orally active CCR4 inhibitor that exhibits an inhibitory effect on the recruitment of Th2 inflammatory immune cells to inflammatory tissues and plays an important role in diseases such as atopic dermatitis, asthma and allergic inflammation.

AF-399 42018025 is a CC chemokine receptor 4 (CCR4) antagonist.

APC-3316 hydrochloride is a vinyl sulfone cysteine protease inhibitor and selective CCR4 antagonist.

APC-3316 tosylate is a vinyl sulfone cysteine protease inhibitor and selective CCR4 antagonist.

GSK2239633 is a potent CC-chemokine receptor 4 antagonist with pIC50 of 7.9. The CC-chemokine receptor 4 (CCR4) is thought potentially to play a critical role in asthma pathogenesis due to its ability to recruit type 2 T-helper lymphocytes to the inflamed airways. Therefore, CCR4 provides an excellent target for anti-inflammatory therapy.

Tivumecirnon (FLX475) is a potent CCR4 antagonist that effectively inhibits regulatory T cells, which hinder antitumor immune responses, thereby demonstrating significant antitumor activity.

CKLF1-C27, a C-terminal peptide of CKLF1, effectively binds to and activates the CCR4 receptor, triggering the ERK1 2 pathway. Competing with CKLF1 for the CCR4 receptor, it neutralizes CKLF1's cellular effects. Additionally, CKLF1-C27 significantly promotes the proliferation of HUVECs and holds promise for psoriasis research [1].

CKLF1-C27 TFA, a C-terminal peptide of CKLF1, binds to the CCR4 receptor and activates the ERK1 2 pathway. It can abrogate the effect of CKLF1 on cells by competing for the CCR4 receptor and shows significant effects on promoting proliferation in HUVECs. CKLF1-C27 TFA has the potential for psoriasis research [1].

CKLF1-C19, the C-terminal peptide of human chemokine-like factor 1 (CKLF1), interacts with CCR4 and inhibits chemotaxis induced by CKLF1 and CCL17. It also suppresses allergic lung inflammation by inhibiting chemotaxis mediated by CCR3 and CCR4 [1].