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(2R,3R,4R,5R)-2-[(1-ethylphosphonyl)-1,1-difluoromethyl]-3,4-dihydroxy-5-hydroxymethyl-pyrrolidine
-
IC50: 1.6 mM
(2R,3R,4R,5S)-2-[(1-ethylphosphonyl)-1,1-difluoromethyl]-3,4-dihydroxy-5-hydroxymethyl-pyrrolidine
-
IC50: 38 mM
(2S,3R,4R,5R)-2-[(1-ethylphosphonyl)-1,1-difluoromethyl]-3,4-dihydroxy-5-hydroxymethyl-pyrrolidine
-
IC50: 4.0 mM
1-(2,2-dibutyl-5-(3,5-dimethylphenyl)-1,3,4-oxadiazol-3(2H)-yl)ethanone
-
0.25 mM, about 30% residual activity
1-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetyl)pyrrolidine-2-carboxylic acid
-
75.5% inhibition at 0.3 mg/ml
1-Geranyl-2-methylbenzimidazole
-
weak
1-[2,2-dibutyl-5-(2-chlorophenyl)-1,3,4-oxadiazol-3(2H)-yl]ethanone
-
0.25 mM, about 10% residual activity
1-[2,2-dibutyl-5-(4-chlorophenyl)-1,3,4-oxadiazol-3(2H)-yl]ethanone
-
0.25 mM, about 30% residual activity
1-[2,2-dibutyl-N-[(2,6-difluorophenyl)carbonyl]-5-(3,5-dimethylphenyl)-1,3,4-oxadiazol-3(2H)-yl]ethanone
-
0.25 mM, about 20% residual activity
1-[2,2-dibutyl-N-[(2-chlorophenyl)carbonyl]-5-(2,4-dichlorophenyl)-1,3,4-oxadiazol-3(2H)-yl]ethanone
-
0.25 mM, about 15% residual activity
1-[2,2-dibutyl-N-[(2-chlorophenyl)carbonyl]-5-(3,5-dimethylphenyl)-1,3,4-oxadiazol-3(2H)-yl]ethanone
-
0.25 mM, about 25% residual activity
2,2'-methylenebis(3,4,6-trichlorophenol)
-
0.25 mM, 56% inhibition
2,3,5,6-Tetrachloro-4-methoxyphenol
-
0.25 mM, 48% inhibition
2,5-dideoxy-2,5-imino-D-glucitol
-
IC50: 5.7 mM
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N,N-dipropylacetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-(2-nitrophenyl)acetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-(3-nitrophenyl)acetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-(4-(trifluoromethyl)phenyl)acetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-(4-methoxyphenyl)acetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-(4-nitrophenyl)acetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-(ptolyl)acetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-methyl-N-phenylacetamide
-
-
2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)-N-phenylacetamide
-
-
2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-3-(4-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetoxy)phenyl)propanoic acid
-
65.3% inhibition at 0.3 mg/ml
2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-3-phenylpropanoic acid
-
-
2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)-4-(methylthio)butanoic acid
-
-
2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)acetic acid
-
-
2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid
-
-
2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
-
3,5-Dichloro-4-methoxybenzaldehyde
-
0.25 mM, 17% inhibition
3,5-Dichloro-4-methoxybenzyl alcohol
-
0.25 mM, 40% inhibition
3,5-Dichlorobenzyl alcohol
-
0.25 mM, 15% inhibition
3-(1H-imidazol-5-yl)-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
61.5% inhibition at 0.3 mg/ml
3-(1H-indol-3-yl)-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
-
3-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
-
3-(2-hydroxy-3-(methyl(2-oxo-2-(piperidin-1-yl)ethyl)amino)propyl)-1-methylquinazoline-2,4(1H,3H)-dione
-
-
3-hydroxy-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)propanoic acid
-
-
3-methyl-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid
-
-
4-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)butanoic acid
-
68.2% inhibition at 0.3 mg/ml
4-methyl-2-(2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)acetamido)pentanoic acid
-
-
5'-(N-succinyl)-5'-amino-5'-deoxyuridine
-
-
-
5'-(N-succinyl)-5'-amino-5'-deoxyuridine methyl ester
-
inhibits the yeast enzyme, and exhibits synergistic interaction with caspofungin against Candida albicans
-
5'-(N-succinylglycyl)-5'-amino-5'-deoxyuridine
-
-
5'-(N-succinylglycyl)-5'-amino-5'-deoxyuridine methyl ester
-
-
5'-deoxy-5'-(glycylamino)uridine
-
-
-
5-(4-(2-hydroxy-3-((2-methoxyphenyl)amino)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-((4-methoxyphenyl)amino)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(1H-imidazol-1-yl)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(4H-1,2,4-triazol-4-yl)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(naphthalen-1-ylamino)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(o-tolylamino)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(p-tolylamino)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(phenylamino)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(piperazin-1-yl)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(piperidin-1-yl)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-(pyrrolidin-1-yl)propyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(2-hydroxy-3-morpholinopropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-((2,6-dimethylphenyl)amino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-((2-chlorophenyl)amino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-((4-bromophenyl)amino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-((4-chlorobenzyl)amino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-((4-chlorophenyl)amino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-(azepan-1-yl)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-(benzylamino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-(bis(2-hydroxyethyl)amino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-(butylamino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-(diethylamino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-(4-(3-(tert-butylamino)-2-hydroxypropyl)piperazin-1-yl)-2-oxo-1,2,3,4-tetrahydroquinoline hydrochloride
-
-
5-[(3,6,6-trimethylhept-4-yn-1-yl)amino]quinolin-2(1H)-one
-
-
5-[(6,6-dimethylhepta-2,4-diyn-1-yl)(methyl)amino]-3,4-dihydroquinolin-2(1H)-one
-
-
8,20-dihydroxy-9(11),13-abietadien-12-one
8-[(6,6-dimethylhepta-2,4-diyn-1-yl)(methyl)amino]-2H-1,4-benzoxazin-3(4H)-one
-
-
amphotericin
-
noncompetitive
Amphotericin B methyl ester
-
-
Ba2+
-
10 mM, 61% inhibition
bis(5'-amino-5'-deoxyuridine) 2,2'-[(1,4-dioxobutane-1,4-diyl)diazanediyl]diacetate
-
50% inhibition at 3 mM
bis(5'-amino-5'-deoxyuridine) 4-[(carboxymethyl)amino]-4-oxobutanoate
-
-
bis(5'-amino-5'-deoxyuridine) succinate
-
-
c3',5'-AMP
-
2 mM, slight inhibition
Calcofluor white
-
noncompetitive
Cd2+
-
complete inhibition of wild-type and mutant enzymes
chitin oligosaccharides
-
slight
edifenphos
-
non-competitive
Hexachlorophene
-
inhibition can be reversed by lecithin
insecticidal benzoylphenyl ureas
-
-
-
K+
-
10 mM, 14% inhibition
kanakugiol
-
inhibition of chitin synthase 2 and antifungal activity of the lignan from the stem bark of Lindera erythrocarpa, overview
linderone
-
inhibition of chitin synthase 2 and antifungal activity of the lignan from the stem bark of Lindera erythrocarpa, overview
methyl 2-((2-(methyl(2-oxo-2H-chromen-4-yl)amino)ethoxy) (phenoxy)phosphorylamino)-3-phenylpropanoate
-
-
methyl 2-((2-(methyl(2-oxo-2H-chromen-4-yl)amino)ethoxy) (phenoxy)phosphorylamino)acetate
-
-
methyl 2-((2-(methyl(2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)propanoate
-
-
methyl 2-((2-(methyl(6-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)-3-phenylpropanoate
-
-
methyl 2-((2-(methyl(6-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)acetate
-
-
methyl 2-((2-(methyl(6-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)propanoate
-
-
methyl 2-((2-(methyl(6-tert-butyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)-3-phenylpropanoate
-
a noncompetitive inhibitor against chitin synthase
methyl 2-((2-(methyl(6-tert-butyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)acetate
-
-
methyl 2-((2-(methyl(6-tert-butyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)propanoate
-
-
methyl 2-((2-(methyl(7-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)-3-phenylpropanoate
-
-
methyl 2-((2-(methyl(7-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)-acetate
-
-
methyl 2-((2-(methyl(7-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)propanoate
-
-
methyl 2-((2-(methyl(8-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)-3-phenylpropanoate
-
-
methyl 2-((2-(methyl(8-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)-acetate}
-
-
methyl 2-((2-(methyl(8-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)propanoate
-
-
methyl 2-(2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)acetamido)benzoate
-
-
methyl 3-methyl-2-((2-(methyl(2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)butanoate
-
-
methyl 3-methyl-2-((2-(methyl(6-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)butanoate
-
-
methyl 3-methyl-2-((2-(methyl(6-tert-butyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)butanoate
-
-
methyl 3-methyl-2-((2-(methyl(7-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)butanoate
-
-
methyl 3-methyl-2-((2-(methyl(8-methyl-2-oxo-2H-chromen-4-yl)amino)ethoxy)(phenoxy)phosphorylamino)butanoate
-
-
methyllinderone
-
inhibition of chitin synthase 2 and antifungal activity of the lignan from the stem bark of Lindera erythrocarpa, overview
N,N'-diacetylchitobiose
-
-
N,N-dibenzyl-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl) (methyl) amino)acetamide
-
-
N,N-diethyl-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl) (methyl) amino)acetamide
-
-
N- benzyl-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl) amino)acetamide
-
-
N-(2-chlorophenyl)-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)acetamide
-
-
N-(4-(cyanomethyl)phenyl)-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)acetamide
-
-
N-(4-chlorobenzyl)-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)acetamide
-
-
N-(4-chlorophenyl)-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl)amino)acetamide
-
-
N-(tert-butyl)-2-((2-hydroxy-3-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)propyl)(methyl) amino)acetamide
-
-
N-acetyl-D-glucosamine
-
-
N1-(2-bromophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
39.9% inhibition at 0.3 mg/ml
N1-(2-chlorophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
46.7% inhibition at 0.3 mg/ml
N1-(2-fluorophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
48.9% inhibition at 0.3 mg/ml
N1-(2-methoxyphenyl)-N4-(2-oxo-12,3,4-tetrahydroquinolin-3-yl) fumaramide
-
82.3% inhibition at 0.3 mg/ml
N1-(2-nitrophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
53.3% inhibition at 0.3 mg/ml
N1-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-N4-(p-tolyl)fumaramide
-
58.7% inhibition at 0.3 mg/ml
N1-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl)-N4-phenylfumaramide
-
35.7% inhibition at 0.3 mg/ml
N1-(3,4-difluorophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
66.5% inhibition at 0.3 mg/ml
N1-(3,5-dimethylphenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
71.5% inhibition at 0.3 mg/ml
N1-(3-bromophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
45.2% inhibition at 0.3 mg/ml
N1-(3-nitrophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
49.3% inhibition at 0.3 mg/ml
N1-(4-bromophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
40.3% inhibition at 0.3 mg/ml
N1-(4-chlorophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
50.5% inhibition at 0.3 mg/ml
N1-(4-fluorophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
51.2% inhibition at 0.3 mg/ml
N1-(4-methoxyphenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
74.6% inhibition at 0.3 mg/ml
N1-(4-nitrophenyl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
65.2% inhibition at 0.3 mg/ml
N1-(naphthalen-1-yl)-N4-(2-oxo-1,2,3,4-tetrahydroquinolin-3-yl) fumaramide
-
27.8% inhibition at 0.3 mg/ml
NaCl
-
0.5 M, 86% inhibition of Chs1 and 29% inhibition of Chs2
oudemansin B
-
0.25 mM, 31% inhibition
Pentachlorophenol
-
0.25 mM, 67% inhibition
Primulin
-
noncompetitive
strobilurin A
-
0.25 mM, 24% inhibition
strobilurin B
-
0.25 mM, 29% inhibition
terpenoyl benzimidazole
-
weak
UDPgalacturonic acid
-
1 mM, about 20% inhibition
UDPglucose
-
1 mM, about 20% inhibition
UDPglucuronic acid
-
1 mM, about 20% inhibition
UDPmannose
-
1 mM, about 20% inhibition
UDPxylose
-
1 mM, about 20% inhibition
uracil polyoxin C methyl ester
[5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl]-carbamic acid 2-[5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethylcarbamoyloxy]-ethyl ester
-
1 mM, 32% inhibition, competitive. IC50: 2.2 mM
[5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethyl]-carbamic acid 2-{2-[5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-3,4-dihydroxy-tetrahydro-furan-2-ylmethylcarbamoyloxy]-ethoxy}-ethyl ester
-
1 mM 45% inhibition. IC50: 11.8 mM
8,20-dihydroxy-9(11),13-abietadien-12-one
-
8,20-dihydroxy-9(11),13-abietadien-12-one
a diterpene compoud isolated from leaves of Chamaecyparis pisifera, inhibits Chs1p; a diterpene compoud isolated from leaves of Chamaecyparis pisifera, inhibits Chs2p
ADP
-
6.25 mM
ADP
-
2.0 mM, 14% inhibition
ATP
-
6.25 mM
ATP
-
2.0 mM, 12% inhibition
Ca2+
-
5-10 mM
Ca2+
-
10 mM, 60% inhibition
Captan
-
-
Co2+
-
10 mM CoCl2, 20% inhibition
Co2+
-
strongly inhibits chitin synthase 1
Co2+
-
inhibits the wild-type Chs2 and mutant Chs2DELTAN222
Cu2+
-
10 mM CuSO4, 95% inhibition
Cu2+
Apodachlya sp.
-
strong
Cu2+
-
10 mM, 47% inhibition
Diflubenzuron
-
slight in vitro inhibition
EDTA
-
10 mM, complete inhibition
EDTA
-
0.1 mM, Chs1 and Chs2 are almost completely inhibited
EDTA
-
inhibition of chitin synthase 1 and 2
EDTA
-
complete inhibition of wild-type and mutant enzymes
Fe3+
-
-
Fe3+
-
10 mM, 71% inhibition
Mg2+
-
low concentration of Mg2+ at 1.0-4.0 mmol/l significantly increase CHS activity, whereas 10.0 mmol/l or higher significantly inhibit CHS enzyme activity
Mg2+
-
inhibits the wild-type Chs2
Mn2+
-
2.5 mM, 50% inhibition of chitin synthase 1 and 2
Mn2+
-
10 mM, 12% inhibition
Ni2+
-
inhibition of chitin synthase 1 and 2, no inhibition of chitin synthase 3
Ni2+
-
inhibits the wild-type enzyme and mutant Chs2DELTAN222
Nikkomycin
-
nikkomycin X and nikkomycin Z
Nikkomycin
-
nikkomycin Z
Nikkomycin
-
nikkomycin Z
Nikkomycin
Kluyveromyces bulgaricus
-
0.015 for chitin synthetase III; IC50: 0.022 mM for chitin synthetase II; IC50: 0.032 mM for chitin synthetase I
Nikkomycin
-
linear competitive inhibitor
Nikkomycin
-
competitive; competitive inhibitor of chitin synthetase 2; nikkomycin X and nikkomycin Z; nikkomycin Z is more inhibitory to chitin synthetase 1 than for chitin synthetase 2
Nikkomycin
-
nikkomycin Z
nikkomycin Z
-
slight in vitro inhibition
nikkomycin Z
exposure to nikkomycin Z, a CHS inhibitor, reduces the amount of chitin in the peritrophic membrane of molted larvae
nikkomycin Z
a chitin synthase inhibitor that downregulates the expression of BmChsA and decreases the amount of epidermis chitin during the molting process
nikkomycin Z
specific for Chs1
nikkomycin Z
competitive inhibition, presence of inhibitor leads to increased expression; competitive inhibition, presence of inhibitor leads to increased expression
O-methyl pisiferic acid
a diterpene compound isolated from leaves of Chamaecyparis pisifera, inhibition of chitin synthase 1
O-methyl pisiferic acid
a diterpene compound isolated from leaves of Chamaecyparis pisifera, specifically inhibits Chs2p in a mixed competitive manner versus UDP-N-acetyl-beta-D-glucosamine
Polyoxin B
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Polyoxin B
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87.5% inhibition at 0.3 mg/ml
Polyoxin B
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85.1% inhibition at 0.3 mg/ml
Polyoxin D
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0.01 mM, 80% loss of activity; 0.1 mM, complete inhibition
Polyoxin D
Apodachlya sp.
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Polyoxin D
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no inhibition
Polyoxin D
Mortierella candelabrum
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Polyoxin D
Mortierella pusilla
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Polyoxin D
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linear competitive inhibitor
Polyoxin D
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Chs2 shows less sensitivity to inhibition than Chs1
Polyoxin D
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competitive inhibitor of chitin synthetase 2; more inhibitory to chitin synthetase 1 than for chitin synthetase 2
polyoxin L
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UDP
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0.05 mM, 50% loss of activity; 0.1 mM, 95% inhibition
UDP
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2.0 mM, 86% inhibition
UDP
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linear competitive inhibitor
UDP
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competitive with respect to UDP-GlcNAc
UDP
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0.5 mM, 28% inhibition
uracil polyoxin C methyl ester
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stereoselective synthesis routes of both the natural (C5'-S) and unnatural (C5'-R) diastereoisomers of uracil polyoxin C methyl ester as specific substrate analogue-inhibitors of chirin synthase, conjugation of the methyl ester of uracil polyoxin C with activated isoxazole carboxylic acids, detailed overview
uracil polyoxin C methyl ester
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stereoselective synthesis routes of both the natural (C5'-S) and unnatural (C5'-R) diastereoisomers of uracil polyoxin C methyl ester as specific substrate analogue-inhibitors of chirin synthase, conjugation of the methyl ester of uracil polyoxin C with activated isoxazole carboxylic acids, detailed overview
UTP
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6.25 mM
UTP
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2.0 mM, 50% inhibition
Zn2+
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10 mM ZnCl2, 95% inhibition
Zn2+
Apodachlya sp.
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strong
Zn2+
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2.5 mM, complete inhibition of both chitin synthase 1 and 2
additional information
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purification of a soluble protein inhibitor from cytoplasm of Mucor rouxii, which forms part of the regulatory mechanism of chitin synthesis in the cells
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additional information
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no in vitro inhibition by polyoxin D. Inhibition of chitin synthesis by the chemicals is not due to direct inhibition of chitin synthase in Anopheles gambiae
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additional information
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synthesis and biological evaluation of phosphoramidate derivatives of coumarin as chitin synthase inhibitors and antifungal agents, overview
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additional information
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synthesis and biological evaluation of novel 3-substituted amino-4-hydroxylcoumarin derivatives as chitin synthase inhibitors and antifungal agents, overview. Most of the compounds have good inhibitory activity against CHS, in which the best compound with IC50 of 0.10 mmol/l has stronger activity than that of polyoxin B As far as the antifungal activity is concerned, most of the compounds possessed moderate to excellent activity against some representative pathogenic fungi. The most potent agent against Cryptococcus neoformans has a minimal inhibitory concentration (MIC) of 0.004 mg/ml. The compounds have negligible actions to some tested bacteria and are promising to develop selective antifungal agents
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additional information
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no inhibition by BAY SIR 8514; no inhibition by diflubenzuron
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additional information
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(2S,3R,4R,5S)-2-[(1-ethylphosphonyl)-1,1-difluoromethyl]-3,4-dihydroxy-5-hydroxymethyl-pyrrolidine shows no inhibition at 8 mM. 2,5-dideoxy-2,5-imino-L-iditol shows no inhibition at 5 mM
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additional information
the absence of Chs4p renders CSIII functionally inactive, independently of Chs3p accumulation at the plasma membrane
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additional information
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the absence of Chs4p renders CSIII functionally inactive, independently of Chs3p accumulation at the plasma membrane
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additional information
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no inhibition of chitin synthase 1 and 3 by methyllinderone, linderone, and kanakugiol from stem bark of Lindera erythrocarpa
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additional information
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design, synthesis and evaluation of 1-methyl-3-substituted quinazoline-2,4-dione derivatives as chitin synthase inhibitors and antifungal agents, NMR and mass spectrometry structure analysis, overview
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additional information
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no inhibition by diflubenzuron
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additional information
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no inhibition by BAY SIR 8514; no inhibition by diflubenzuron
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additional information
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a pH-dependent, heat-stable inhibitor is present in the soluble cytoplasm from the mycelium
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