chitinase-in-2

Chitinase-IN-2 is an insect chitinase and N- acetyl hexosaminidase inhibitor and pesticide.

Chitinase-IN-2 hydrochloride functions as an inhibitor of both insect chitinase and N-acetyl hexosaminidase, and also serves as a pesticide. At concentrations of 50 µM and 20 µM, it demonstrates inhibitory effectiveness of 98% and 92% against chitinase and N-acetyl-hexosaminidase, respectively.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.

Argadin, a cyclopentapeptide chitinase inhibitor, effectively inhibits chitinase B (ChiB) with a K i value of 20 nM. It holds potential for research in fungicide and insecticide applications [1] [2].

EP4 antagonist 14 is a prostaglandin E2 receptor subtype EP4 antagonist, demonstrating an IC50 of 1.1 nM in a HEK293 human receptor reporter assay and blocking β-arrestin recruitment due to PGE2 with an IC50 of 0.9 nM. At 10 µM, it reduces PGE2-stimulated mRNA levels of Il-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1) in RAW 264.7 macrophages. When used at 30 mg/kg per day alongside anti-PD-1 antibodies, it curbs tumor growth and enhances CD8+ T cell infiltration in tumors using a CT26 murine colon cancer model.

K284-6111 is an orally effective inhibitor of the Chitinase 3-like 1 protein (CHI3L1). It functions by reducing the expression of inflammatory proteins such as iNOS, COX-2, GFAP, and Iba-1, and inhibits both β-secretase (β-secretase) and NF-κB, leading to a suppression of Aβ production. Furthermore, K284-6111 improves memory impairment in mice induced by Aβ1–42, making it useful for research in Alzheimers disease.