cxcr2 in 2

CXCR2-IN-2 (compound 68) is a highly selective CXCR2 antagonist (IC50=5.2 nM) with the advantages of blood-brain barrier penetration and oral bioavailability. It inhibits Gro-α-induced CD11b expression in human whole blood (IC50=0.04 μM).

(R,R)-CXCR2-IN-2, a diastereoisomer of CXCR2-IN-2 (compound 68), is a brain-penetrant CXCR2 antagonist with a pIC50 of 9 in the Tango assay and 6.8 in the HWB Gro-α induced CD11b expression assay[1].

CXCR2 antagonist 3 (compound 11h) is a highly effective inhibitor of CXC chemokine receptor 2 (CXCR2), displaying double-digit nanomolar potencies in inhibiting neutrophil infiltration into the air pouch. Additionally, it reduces neutrophil and MDSC infiltration while enhancing CD3+ T lymphocyte infiltration into Pan02 tumor tissues [1].

CXCR2/CCR7 antagonist-1 (compound 6) is a potent dual antagonist of CXCR2 and CCR7, with IC50 values of 0.0046 μM and 0.0014 μM, respectively. It is valuable for research in tumor metastasis and autoimmune diseases.

NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability.

CXCR2 antagonist 8 is a selective CXCR2 antagonist, which can be used for the treatment and prevention of insulin resistance.

CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.013 μM) and effective calcium mobilization (IC50 = 0.1 μM) [1].

CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.044 μM) and calcium mobilization (IC50 = 0.66 μM) [1].

CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist with strong binding affinity (IC50 = 0.044 μM) and effective calcium mobilization (IC50 = 0.66 μM) [1].

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunotherapy, exhibiting an IC50 value of 95 nM.

CXCR2 antagonist 4 (compound 7) is a highly potent inhibitor of CXCR2 with an IC50 of 0.13 μM and effectively inhibits the CXCL8-induced cytosolic calcium increase with an IC50 of 27 μM, demonstrating promising potential for anticancer research [1].

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

Ladarixin (DF 2156A free base) is an orally active, non-competitive CXCR1/CXCR2 allosteric inhibitor that suppresses AKT, NF-κB, and angiogenesis, thereby slowing the progression of experimental human melanoma. It may be employed in research concerning COPD, asthma, and melanoma.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

Corydalmine hydrochloride is a chemical compound that suppresses spore germination in certain plant pathogenic and saprophytic fungi [1], serves as an effective oral analgesic agent with potent activity [2], and mitigates Vincristine-induced neuropathic pain in mice through the inhibition of an NF-κB-dependent CXCL1/CXCR2 signaling pathway [3].