chitinase

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] .

Closantel (R-31520), a salicylanilide anthelmintic compound, shows different anthelmintic spectra and obvious toxicity in mammals.

Closantel is a salicylanilide anthelmintic compound; exhibits different anthelmintic spectra and apparent toxicity in mammals.

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

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.

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.

Chitinase-IN-6 (Compound 4h) is an effective dual-Chitinase inhibitor, exhibiting Ki values of 1.82 μM and 2.00 μM against OfChtI and OfChi-h, respectively. It has a growth inhibitory effect on the Asian corn borer (Ostrinia furnacalis) and is a promising new insecticide candidate that is friendly to non-target organisms.

Chitinase-IN-4 (compound 8f) is a potent and selective inhibitor of OfChi-h with an IC50 value of 0.1 μM, exhibiting strong insecticidal activity.

Chitinase-IN-5 (8i) is a potent inhibitor of chitinase OfChi-h (IC50: 0.051 μM) with significant insecticidal properties. It can be utilized for research in green pest control and management.

Dibenzylideneacetone (DBA) is an antifungal agent that exhibits inhibitory activity against Botrytis cinerea Chitinase with an IC50 of 13.10 µg mL. It has a minimum inhibitory concentration (MIC) against B. cinerea of 32 µg mL. The EC50 values for inhibiting mycelial growth and spore germination are 16.29 µg mL and 14.64 µg mL, respectively. Dibenzylideneacetone effectively combats grey mold infection in cherry tomatoes by inhibiting chitinase activity.

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.

Insecticidal agent 9 (Compound I-17) is an insecticide with strong pest control properties. It exhibits LC50 values of 93.32 mg/L and 114.79 mg/L against Plutella xylostella and Ostrinia furnacalis, respectively. At a concentration of 500 mg/L, it achieves an 86.1% mortality rate for Spodoptera frugiperda. The compound effectively targets ecdysone receptors (EcR) and three chitinase enzymes (OfChtI, OfChtII, and OfChi-h), demonstrating excellent binding activity with EcR and inhibition rates for the chitinases. Insecticidal agent 9 is suitable for research in pest management.

Allosamidin, a chitinase inhibitor and typical secondary metabolite of Streptomyces, may be used as a pesticide and anti-asthmatic agent.

Chitopentaose pentahydrochloride is an anti-inflammatory chitosan oligosaccharide that functions as a substrate for the gene encoding chitinase B (FjchiB).

Bisdionin C is a potent inhibitor of GH18 chitinase with an IC50 of 0.2 μM for A. fumigatus ChiB1. Bisdionin C inhibits human macrophage chitotriosidase(HCHT, IC50 = 8.3 μM) and acidic mammalian chitinase (AMCase, IC50 = 3.4 μM).

Lynamicin B, a promising pesticide, functions as a selective chitinase inhibitor exclusive to lepidoptera. It exhibits a Ki value of 8.76 μM, indicating its potential efficacy.

OAT-177 is a potent, selective, orally active acidic mammalian chitinase (AMCase) inhibitor.

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.

Glucoallosamidin A is a glycoside antibiotic that inhibits chitinase activity. It effectively suppresses the chitinase enzyme in Candida albicans [ATCC 10231], exhibiting an IC50 of 3.4 μg/mL.