KF38789

• CAT Number: I010623
• CAS Number: 257292-29-8
• Molecular Formula: C19H21NO5S
• Molecular Weight: 375.44
• Purity: ≥95%
• Synonyms: 3-[7-(2,4-dimethoxyphenyl)-2,3,6,7-tetrahydro-1,4-thiazepin-5-yl]-4-hydroxy-6-methylpyran-2-one
• InChI: InChI=1S/C19H21NO5S/c1-11-8-15(21)18(19(22)25-11)14-10-17(26-7-6-20-14)13-5-4-12(23-2)9-16(13)24-3/h4-5,8-9,17,21H,6-7,10H2,1-3H3
• InChIKey: NHFIAAAMCYVRIW-UHFFFAOYSA-N
• SMILES: CC1=CC(=C(C(=O)O1)C2=NCCSC(C2)C3=C(C=C(C=C3)OC)OC)O

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].
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].

Reference

[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.
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[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.
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[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.
 [Content Brief]