chitinase 1

Chitinase-IN-1 is an inhibitor of insect chitinases and N-acetylhexosaminidases that does not inhibit N-acetylhexosaminidases of mammalian and plant origin, and can be used as an insecticide.

OATD-01 is a highly active inhibitor of both Chitotriosidase (CHIT1) and acidic mammalian chitinase (AMCase).

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.

CHI3L1-IN-5 (Compound Z17) is a highly selective small-molecule inhibitor that targets chitinase-like 1 (CHI3L1). CHI3L1-IN-5 alleviates neuroinflammation by inhibiting the NF-κB pathway. CHI3L1-IN-5 can be used in research on inflammation, fibrosis, Alzheimer’s disease, and tumors.

CHI3L1-IN-4 (Compound 8) is an inhibitor of chitinase-3-like protein 1 (CHI3L1), exhibiting a Kd of 6.8 μM. By disrupting the CHI3L1 pathway, CHI3L1-IN-4 significantly reduces the viability of glioblastoma (GBM) spheres and lowers phosphorylated STAT3 levels. This compound is applicable in GBM research.

Chitinase has partial lysozyme activity and is widely found in bacteria, fungi, animals and some plants . Chitinase belongs to the glycosyl hydrolase family. Chitinase catalyzes chito-oligosaccharide hydrolysis [1] .

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].

ZK-PI-9 acts as an inhibitor of both trehalase and chitinase activities in female pupae and functions as an insecticide [1].

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.

CHI3L1-IN-1 (Compound 30), a potent inhibitor of Chitinase-3-like protein 1 (CHI3L1) (YKL-40), exhibits an IC 50 of 50 nM. Additionally, this compound displays inhibitory activity against the hERG channel with an IC 50 of 2.3 μM [1].

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.

Argifin is a chitinase inhibitor produced by the metabolism of soil microorganisms, with inhibitory activity at the sub-nanomolar level; its IC50 values against Serratia marcescens chitinase A and B, Aspergillus fumigatus chitinase B1 and human chitotriosidase are 0.025 μM, 6.4 μM, 1.1 μM and 4.5 μM, respectively [1].

Cyclo(Arg-Pro) (Cyclo(Pro-Arg)), a chitinase inhibitor, prevents the cell separation of Saccharomyces cerevisiae without impacting its growth. Additionally, it restricts the morphological transformation of Candida albicans from its yeast form to a filamentous form [1].