KF38789

KF38789 is a selective inhibitor of P-selectin-PSGL-1 binding. KF38789 inhibits the binding of U937 cells to immobilized P-selectin immunoglobulin G chimeric protein (P-selectin-Ig) with an IC50 value of 1.97 μM[1].

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

KF38789 inhibits P-selectin-induced superoxide production from human polymorphonuclear cells. Intravenously injected KF38789 significantly inhibits the thioglycollate (TG)-induced accumulation of leukocytes in the mouse peritoneal cavity[1]. KF38789 displays a concentration-dependent inhibition of U937 cell adhesion to immobilized P-selectin-Ig with an IC50 value of 1.97±0.74 μM[1]. KF38789 specifically inhibits P-selectin-dependent cell adhesion and the leukocyte recruitment in mouse peritonitis[1]. KF38789 (5 μM) significantly reduces closure of a 500-μm gap between confluent sheets of Human corneal epithelial (HCE)-T cells over an 8-hr period (by ∼40%)[2]. Corneal epithelial cell migration is reduced in the presence of KF38789 (5 μM) [2].

KF38789 can block P-selectin-mediated binding in vitro and leukocyte accumulation in vivo[1]. Intraperitoneal injection of the P-selectin inhibitor KF38789 (daily intraperitoneal injection of 10mg/kg for 12 days) significantly reduces mechanical allodynia in the facial carrageenan-injected mice[3]. Animal Model: BALB/c mice[1] Dosage: 1 mg/kg Administration: Intravenously administrated Result: Significantly reduced leukocyte accumulation. Animal Model: Twenty-four adult male C57BL/6J (B6) mice, about 6-8 weeks of age and weighing approximately 20-30 g[3] Dosage: 10 mg/kg, 1 mg/kg, 0.1 mg/kg, 0.01 mg/kg or 0.001 mg/kg Administration: Intraperitoneal injection daily for 12 days Result: Significantly reduced mechanical allodynia in the facial carrageenan-injected mice.

[1]. S Ohta, et al. Inhibition of P-selectin specific cell adhesion by a low molecular weight, non-carbohydrate compound, KF38789. Inflamm Res. 2001 Nov;50(11):544-51.

[2]. Peter J Gillies, et al. Demonstration of P-selectin expression and potential function in human corneal epithelial cells. Exp Eye Res. 2018 Nov;176:196-206.

[3]. Kay-Wee Poh, et al. Global gene expression analysis in the mouse brainstem after hyperalgesia induced by facial carrageenan injection--evidence for a form of neurovascular coupling? Pain. 2009 Mar;142(1-2):133-41.