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抑制剂

抑制剂简介

抑制剂是一类能够降低或阻止生物体内的酶活性、受体的活性或是细胞内特定反应过程的小分子化合物。它们在有机化学、化学化工和生物医药领域中有着广泛的应用,尤其是在药物研发方面。

分类与作用机制

  1. 竞争性抑制剂:这类抑制剂通过与其目标蛋白质(如酶)结合,占据其底物结合位点,从而阻止真正的底物与蛋白质的正常结合。这种类型的抑制通常可以通过增加底物浓度来缓解。
  2. 非竞争性抑制剂:非竞争性抑制剂通过改变蛋白质的功能状态或结构,而不直接与其活性部位相结合。它们可能会影响蛋白质的构象变化或者与其他位点相互作用。
  3. 不可逆抑制剂:这类抑制剂与酶或其他生物分子形成共价键,导致其永久失去功能。由于这种特性,此类抑制剂通常用于实验室研究中。

应用领域

  1. 药物开发:在生物医药领域,抑制剂被广泛用作潜在的治疗药物,用于对抗各种疾病如癌症、病毒感染等。
  2. 酶学研究:有机化学和生物化学研究经常使用特定类型的抑制剂来探究酶的功能和作用机理。
  3. 合成与催化:化学化工中,通过调节反应条件或引入适当的抑制剂可以提高某些目标产物的选择性。

总结

抑制剂的研究和发展对于理解生命过程至关重要,并在药物开发、基础科学研究等多个领域发挥着重要作用。随着技术的进步,新的抑制剂不断被发现和开发出来,为医学治疗提供了更多的可能性。

中文名称 英文名称 CAS号 化学式 结构式图片
—— (1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone 137071-32-0 C43H68ClNO11
(1R,9S,12S,13R,14S,17R,21S,23S,24R,25S,27R)-12-[(E)-1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
—— Ambap5429 104987-11-3 C44H69NO12
Ambap5429
—— Benz(g)isoquinoline-5,10-dione, 6,9-bis((2-aminoethyl)amino)-, (2Z)-2-butenedioate (1:2) 144675-97-8 C25H27N5O10
Benz(g)isoquinoline-5,10-dione, 6,9-bis((2-aminoethyl)amino)-, (2Z)-2-butenedioate (1:2)
—— (3E)-5-chloro-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one 1055412-47-9 C15H13ClN2O
(3E)-5-chloro-3-[(3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-1H-indol-2-one
—— (Z)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide 257933-82-7 C24H23ClFN5O2
(Z)-N-[4-(3-chloro-4-fluoroanilino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
—— 2-[8-(2,4-Dichlorophenyl)-2-hydroxyoctyl]-2-hydroxybutanedioic acid 154566-12-8 C18H24Cl2O6
2-[8-(2,4-Dichlorophenyl)-2-hydroxyoctyl]-2-hydroxybutanedioic acid
—— Rapivab 330600-85-6 C15H36N4O8
Rapivab
—— (1R,9S,12S,13S,14S,17R,21S,23S,24R,25S,27R)-12-[1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone 137071-32-0 C43H68ClNO11
(1R,9S,12S,13S,14S,17R,21S,23S,24R,25S,27R)-12-[1-[(1R,3R,4S)-4-chloro-3-methoxycyclohexyl]prop-1-en-2-yl]-17-ethyl-1,14-dihydroxy-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
—— 6,9-Bis(2-aminoethylamino)benzo[g]isoquinoline-5,10-dione;but-2-enedioic acid 144675-97-8 C25H27N5O10
6,9-Bis(2-aminoethylamino)benzo[g]isoquinoline-5,10-dione;but-2-enedioic acid
—— 2-[2-Chloro-6-ethoxy-4-[(3-methyl-5-oxo-1-phenyl-4-pyrazolylidene)methyl]phenoxy]acetic acid methyl ester 431979-47-4 C22H21ClN2O5
2-[2-Chloro-6-ethoxy-4-[(3-methyl-5-oxo-1-phenyl-4-pyrazolylidene)methyl]phenoxy]acetic acid methyl ester
—— (1S,4S,7Z,10S,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone 128517-07-7 C24H36N4O6S2
(1S,4S,7Z,10S,21R)-7-ethylidene-4,21-di(propan-2-yl)-2-oxa-12,13-dithia-5,8,20,23-tetrazabicyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone
—— 1-(2,6-dimethyl-1H-indol-3-yl)-2-[4-(furan-2-carbonyl)piperazin-1-yl]ethanone 371210-26-3 C21H23N3O3
1-(2,6-dimethyl-1H-indol-3-yl)-2-[4-(furan-2-carbonyl)piperazin-1-yl]ethanone
—— 5-[(4-Ethylphenyl)methylene]-2-thioxo-4-thiazolidinone 403811-55-2 C12H11NOS2
5-[(4-Ethylphenyl)methylene]-2-thioxo-4-thiazolidinone
—— 2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-(5-quinolinyl)-2-propenamide 304896-28-4 C23H13Cl2N3O2
2-cyano-3-[5-(2,5-dichlorophenyl)-2-furanyl]-N-(5-quinolinyl)-2-propenamide
—— Isrib 1597403-47-8 C22H24Cl2N2O4
Isrib
—— 1-(3-Ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one 300801-52-9 C13H15NO2S
1-(3-Ethyl-5-methoxy-1,3-benzothiazol-2-ylidene)propan-2-one
—— 4,4'-(Furan-2,5-diyl)dibenzimidamide dihydrochloride 55368-40-6 C18H18Cl2N4O
4,4'-(Furan-2,5-diyl)dibenzimidamide dihydrochloride
—— Tautomycin 109946-35-2 C41H66O13
Tautomycin
—— [(3R,4R,5S,8S,9S,12R)-12-[(2S,3S,6R,8S,9R)-3,9-dimethyl-8-[(3S)-3-methyl-4-oxopentyl]-1,7-dioxaspiro[5.5]undecan-2-yl]-5,9-dihydroxy-4-methoxy-2,8-dimethyl-7-oxotridecan-3-yl] (3R)-3-hydroxy-3-(4-methyl-2,5-dioxofuran-3-yl)propanoate 109946-35-2 C41H66O13
[(3R,4R,5S,8S,9S,12R)-12-[(2S,3S,6R,8S,9R)-3,9-dimethyl-8-[(3S)-3-methyl-4-oxopentyl]-1,7-dioxaspiro[5.5]undecan-2-yl]-5,9-dihydroxy-4-methoxy-2,8-dimethyl-7-oxotridecan-3-yl] (3R)-3-hydroxy-3-(4-methyl-2,5-dioxofuran-3-yl)propanoate
—— [(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24Z,26E,28E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate 162635-04-3 C56H87NO16
[(1R,2R,4S)-4-[(2R)-2-[(1R,9S,12S,15R,16E,18R,19R,21R,23S,24Z,26E,28E,30S,32S,35R)-1,18-dihydroxy-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-2,3,10,14,20-pentaoxo-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraen-12-yl]propyl]-2-methoxycyclohexyl] 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate
—— (1S,4E,5'R,6R,6'R,7S,8R,10S,11R,12R,14R,15R,16S,18E,20E,22S,25S,27S,28R,29S)-22-ethyl-7,11,15-trihydroxy-6'-[(2S)-2-hydroxypropyl]-5',6,8,10,12,14,16,28,29-nonamethylspiro[2,26-dioxabicyclo[23.3.1]nonacosa-4,18,20-triene-27,2'-oxane]-3,9,13-trione 11052-72-5 C45H74O10
(1S,4E,5'R,6R,6'R,7S,8R,10S,11R,12R,14R,15R,16S,18E,20E,22S,25S,27S,28R,29S)-22-ethyl-7,11,15-trihydroxy-6'-[(2S)-2-hydroxypropyl]-5',6,8,10,12,14,16,28,29-nonamethylspiro[2,26-dioxabicyclo[23.3.1]nonacosa-4,18,20-triene-27,2'-oxane]-3,9,13-trione
—— (1S,9R,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone 104987-11-3 C44H69NO12
(1S,9R,12S,13R,14S,17R,18E,21S,23S,24R,25S,27R)-1,14-dihydroxy-12-[(E)-1-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
—— (1R,9S,14S,18E,21S,23S,24R)-1,14-dihydroxy-12-[(E)-1-[(3R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone 104987-11-3 C44H69NO12
(1R,9S,14S,18E,21S,23S,24R)-1,14-dihydroxy-12-[(E)-1-[(3R)-4-hydroxy-3-methoxycyclohexyl]prop-1-en-2-yl]-23,25-dimethoxy-13,19,21,27-tetramethyl-17-prop-2-enyl-11,28-dioxa-4-azatricyclo[22.3.1.04,9]octacos-18-ene-2,3,10,16-tetrone
—— Azanide;2-oxidoacetate;platinum(4+) 95734-82-0 C2H6N2O3Pt
Azanide;2-oxidoacetate;platinum(4+)
—— LY2452473 1029692-15-6 C22H22N4O2
LY2452473
—— Hesperadin 422513-13-1 C29H32N4O3S
Hesperadin
—— 2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate 634913-39-6 C15H9ClF6NO5P
2-{[3,5-bis(trifluoromethyl)phenyl]carbamoyl}-4-chlorophenyl dihydrogen phosphate
—— Copanlisib 1032568-63-0 C23H28N8O4
Copanlisib
—— varenicline tartrate 375815-87-5 C4H6O6*C13H13N3
varenicline tartrate
—— (13S,17S)-2-Methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol 362-07-2 C19H26O3
(13S,17S)-2-Methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
—— AMG176 1883727-34-1 C33H41ClN2O5S
AMG176
—— 3-pentadecylidenepentane-2,4-dione 1314006-43-3 C20H36O2
3-pentadecylidenepentane-2,4-dione
—— chloromethyl (8S,9S,10R,11S,13S,14S,17S)-17-((ethoxycarbonyl)oxy)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylate 82034-46-6 C24H31ClO7
chloromethyl (8S,9S,10R,11S,13S,14S,17S)-17-((ethoxycarbonyl)oxy)-11-hydroxy-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylate
—— 3-[4-[(2R)-2-aminopropoxy]phenyl]-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine 1505514-27-1 C23H24FN5O
3-[4-[(2R)-2-aminopropoxy]phenyl]-N-[(1R)-1-(3-fluorophenyl)ethyl]imidazo[1,2-b]pyridazin-6-amine
—— 5-Methyl-6-(4-pyridinyl)-2H-imidazo(4,5-b)pyridin-2-one 152633-54-0 C12H10N4O
5-Methyl-6-(4-pyridinyl)-2H-imidazo(4,5-b)pyridin-2-one
—— [4-amino-2-[[(1S,2S,4R)-2-bicyclo[2.2.1]heptanyl]amino]-1,3-thiazol-5-yl]-(2-nitrophenyl)methanone 2237942-08-2 C17H18N4O3S
[4-amino-2-[[(1S,2S,4R)-2-bicyclo[2.2.1]heptanyl]amino]-1,3-thiazol-5-yl]-(2-nitrophenyl)methanone
—— OligomycinC 11052-72-5 C45H74O10
OligomycinC
—— Trospium Chloride 10405-02-4 C25H30NO3*Cl
Trospium Chloride
—— 2-Oxidoacetate;platinum(2+) 95734-82-0 C2H2O3Pt
2-Oxidoacetate;platinum(2+)
—— (R)-3-cyclopentyl-N-((S)-3,3-dimethyl-1-oxo-1-(4-((2,4,5-trifluorobenzyl)amino) piperidin-1-yl)butan-2-yl)-2-((N-hydroxyformamido)methyl)propanamide 1091682-50-6 C28H41F3N4O4
(R)-3-cyclopentyl-N-((S)-3,3-dimethyl-1-oxo-1-(4-((2,4,5-trifluorobenzyl)amino) piperidin-1-yl)butan-2-yl)-2-((N-hydroxyformamido)methyl)propanamide
—— 17α-Allyl-17β-hydroxyoestra-4,9,11-trien-3-on 850-52-2 C21H26O2
17α-Allyl-17β-hydroxyoestra-4,9,11-trien-3-on
—— 3-Oxo-17β-hydroxy-17α-allylestra-4,9,11-trien 850-52-2 C21H26O2
3-Oxo-17β-hydroxy-17α-allylestra-4,9,11-trien
—— L156602 125228-51-5 C38H64N8O13
L156602
—— Ammonaps 1716-12-7 C10H11O2*Na
Ammonaps
—— [4-chloro-6-(2,3-xylidino)-2-pyrimidinylthio] acetic acid 50892-23-4 C14H13ClN2O2S
[4-chloro-6-(2,3-xylidino)-2-pyrimidinylthio] acetic acid
—— 2-[4-chloro-6-(2,3-dimethylanilino)pyrimidin-2-yl]acetic acid 50892-23-4 C14H14ClN3O2
2-[4-chloro-6-(2,3-dimethylanilino)pyrimidin-2-yl]acetic acid
—— (4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thioacetic acid 50892-23-4 C14H14ClN3OS
(4-chloro-6-(2,3-xylidino)-2-pyrimidinyl)thioacetic acid
—— gestodene 60282-87-3 C21H26O2
gestodene
—— 11-Benzyl-7-[(2-methylphenyl)methyl]-2,5,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),5-dien-10-one 41276-02-2 C24H26N4O
11-Benzyl-7-[(2-methylphenyl)methyl]-2,5,7,11-tetrazatricyclo[7.4.0.02,6]trideca-1(9),5-dien-10-one
—— N-{(1S,2R)-1-benzyl-3-[(3R,4S)-3,4-dihydroxypyrrolidin-1-yl]-2-hydroxy-3-oxopropyl}-5-chloro-1H-indole-2-carboxamide 186392-65-4 C23H24ClN3O5
N-{(1S,2R)-1-benzyl-3-[(3R,4S)-3,4-dihydroxypyrrolidin-1-yl]-2-hydroxy-3-oxopropyl}-5-chloro-1H-indole-2-carboxamide