chitinase

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 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).

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).

Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms (IC50: 0.025 μM, 6.4 μM, 1.1 μM, and 4.5 μM for SmChiA [Serratia marcescens chitinase A], SmChiB, Aspergillus fumigatus chitinase B1, and human chitotriosidase).

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.

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.

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).

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.