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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
—— 4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid 149709-62-6 C24H29NO5
4-(((2S,4R)-1-([1,1'-biphenyl]-4-yl)-5-ethoxy-4-methyl-5-oxopentan-2-yl)amino)-4-oxobutanoic acid
—— DL-nebivolol hydrochloride 152520-56-4 C22H25F2NO4*ClH
DL-nebivolol hydrochloride
—— 2-(4-ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-1-yl)acetamide 881375-00-4 C33H34N4O4S
2-(4-ethylpiperazin-1-yl)-N-(4-(2-morpholino-4-oxo-4H-chromen-8-yl)dibenzo[b,d]thiophen-1-yl)acetamide
—— Trimethyl-[2-[4-oxo-4-[2-(trimethylazaniumyl)ethoxy]butanoyl]oxyethyl]azanium;chloride;hydrate 6101-15-1 C14H32ClN2O5+
Trimethyl-[2-[4-oxo-4-[2-(trimethylazaniumyl)ethoxy]butanoyl]oxyethyl]azanium;chloride;hydrate
—— Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-,hydrochloride, dihydrate, (5a)- 51481-60-8 C19H24ClNO5
Morphinan-6-one, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-,hydrochloride, dihydrate, (5a)-
—— Blasticidine S hydrochloride 3513-03-9 C17H27ClN8O5
Blasticidine S hydrochloride
—— methyl (4aS,6aR,6bS,12aS,14aR,14bR)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylate 218600-53-4 C32H43NO4
methyl (4aS,6aR,6bS,12aS,14aR,14bR)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,3,4,5,6,7,8,8a,14a,14b-decahydropicene-4a-carboxylate
—— CCI-779 162635-04-3 C56H87NO16
CCI-779
—— (3S,4R,5R,8R,9Z,12R,14S,15R,16S,18R,19R,26aS)-8-allyl-5,19-dihydroxy-3-{(E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylvinyl}-14,16-dimethoxy-4,10,12,18-tetramethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3H-15,19-epoxypyrido[2,1-c][1,4]oxazacyclotricosine-1,7,20,21(4H,23H)-tetrone 104987-11-3 C44H69NO12
(3S,4R,5R,8R,9Z,12R,14S,15R,16S,18R,19R,26aS)-8-allyl-5,19-dihydroxy-3-{(E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylvinyl}-14,16-dimethoxy-4,10,12,18-tetramethyl-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-3H-15,19-epoxypyrido[2,1-c][1,4]oxazacyclotricosine-1,7,20,21(4H,23H)-tetrone
—— Antibiotic S 7481F1 59865-13-3 C62H111N11O12
Antibiotic S 7481F1
—— 4-Pyrimidinamine, 6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-((1E)-2-phenylethenyl)-, (2R,3R)-2,3-dihydroxybutanedioate (1:1) 934353-76-1 C25H31N7O6
4-Pyrimidinamine, 6-(4-methyl-1-piperazinyl)-N-(5-methyl-1H-pyrazol-3-yl)-2-((1E)-2-phenylethenyl)-, (2R,3R)-2,3-dihydroxybutanedioate (1:1)
—— [(Z)-4-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-3-[[(E)-2-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-5-(2-methylpropanoyloxy)pent-2-en-3-yl]disulfanyl]pent-3-enyl] 2-methylpropanoate 3286-46-2 C32H46N8O6S2
[(Z)-4-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-3-[[(E)-2-[(4-amino-2-methylpyrimidin-5-yl)methyl-formylamino]-5-(2-methylpropanoyloxy)pent-2-en-3-yl]disulfanyl]pent-3-enyl] 2-methylpropanoate
—— Nacubactam monohydrate 2007923-17-1 C9H18N4O8S
Nacubactam monohydrate
—— N-[(3S,6S,12R,15S,16R,19S)-25-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]sulfanylmethyl]-3-[[4-(dimethylamino)phenyl]methyl]-12-ethyl-4,16-dimethyl-2,5,11,14,18,21,24-heptaoxo-19-phenyl-17-oxa-1,4,10,13,20-pentazatricyclo[20.4.0.06,10]hexacosan-15-yl]-3-hydroxypyridine-2-carboxamide 120138-50-3 C53H67N9O10S
N-[(3S,6S,12R,15S,16R,19S)-25-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]sulfanylmethyl]-3-[[4-(dimethylamino)phenyl]methyl]-12-ethyl-4,16-dimethyl-2,5,11,14,18,21,24-heptaoxo-19-phenyl-17-oxa-1,4,10,13,20-pentazatricyclo[20.4.0.06,10]hexacosan-15-yl]-3-hydroxypyridine-2-carboxamide
—— 8-Azaspiro[4.5]decane-7,9-dione, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-, hydrochloride (1:2) 21102-95-4 C22H32ClN3O3
8-Azaspiro[4.5]decane-7,9-dione, 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-, hydrochloride (1:2)
—— (1R,9S,12S,13R,14R,17R,18Z,21R,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
(1R,9S,12S,13R,14R,17R,18Z,21R,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
—— Nelfinavir mesylate hydrate 159989-65-8 C33H51N3O8S2
Nelfinavir mesylate hydrate
—— Taniborbactam 1613267-49-4 C19H28BN3O5
Taniborbactam
—— Pco-371 1613373-33-3 C29H32F3N5O6S
Pco-371
—— (2S,3S)-2-(dimethylamino)-N-[(2S)-2-[[(3R,5S)-3-methoxy-1-[(2S)-2-[(2R)-1-methoxy-2-methyl-3-oxo-3-[[(1R)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methylbutanoyl]-3-methylpentanamide 212007-18-6 C43H70N6O6S
(2S,3S)-2-(dimethylamino)-N-[(2S)-2-[[(3R,5S)-3-methoxy-1-[(2S)-2-[(2R)-1-methoxy-2-methyl-3-oxo-3-[[(1R)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methylbutanoyl]-3-methylpentanamide
—— 2-[3-(2,6-Dimethylpiperazin-1-yl)phenyl]-2-phenylpentanamide 149838-21-1 C23H31N3O
2-[3-(2,6-Dimethylpiperazin-1-yl)phenyl]-2-phenylpentanamide
—— {[4-phenyl-1-(4-(2-quinolinylmethoxy)phenyl)butyl]thio}acetic acid 127481-29-2 C28H27NO3S
{[4-phenyl-1-(4-(2-quinolinylmethoxy)phenyl)butyl]thio}acetic acid
—— Sulbutiamine 3286-46-2 C32H46N8O6S2
Sulbutiamine
—— (1S,4S,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,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
—— Azanide;2-hydroxyacetic acid;platinum(2+) 95734-82-0 C2H8N2O3Pt
Azanide;2-hydroxyacetic acid;platinum(2+)
—— Histamine Phosphate 51-74-1 C5H15N3O8P2
Histamine Phosphate
—— Cisatracurium Besylate 96946-42-8 C65H82N2O18S2
Cisatracurium Besylate
—— N,N,N,2-Tetramethyl-5-(1-methylethyl)-4-((1-piperidinylcarbonyl)oxy)benzenaminium chloride 2438-53-1 C19H31ClN2O2
N,N,N,2-Tetramethyl-5-(1-methylethyl)-4-((1-piperidinylcarbonyl)oxy)benzenaminium chloride
—— 4-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-N-(2-methyl-1-(2-(1-methylpiperidin-4-yl)phenyl)propan-2-yl)-6-morpholino-1,3,5-triazin-2-amine 1401436-95-0 C31H38F2N8O
4-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-N-(2-methyl-1-(2-(1-methylpiperidin-4-yl)phenyl)propan-2-yl)-6-morpholino-1,3,5-triazin-2-amine
—— lubiprostone 136790-76-6 C20H32F2O5
lubiprostone
—— (2S)-1-[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]-N-[2-[[(2S)-1-[[2-[[(1R,2S)-1-hydroxy-1-[4-hydroxy-3-(3-methylbut-2-enyl)phenyl]-3-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]-2,3-dihydropyrrole-2-carboxamide 151928-32-4 C41H52N8O9
(2S)-1-[(2S)-2-[(2-aminoacetyl)amino]-3-(1H-indol-3-yl)propanoyl]-N-[2-[[(2S)-1-[[2-[[(1R,2S)-1-hydroxy-1-[4-hydroxy-3-(3-methylbut-2-enyl)phenyl]-3-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-2-oxoethyl]-2,3-dihydropyrrole-2-carboxamide
—— PIK-90 677338-12-4 C18H17N5O3
PIK-90
—— MK2206 dihydrochloride 1032350-13-2 C25H21N5O*2ClH
MK2206 dihydrochloride
—— 3-amino-N-(5-(4-(2,3-dichlorophenyl)piperazin-1-yl)pentyl)-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide 1610591-93-9 C25H31Cl2N5OS
3-amino-N-(5-(4-(2,3-dichlorophenyl)piperazin-1-yl)pentyl)-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide
—— 6-amino-8-trifluoromethylphenanthridine 651055-83-3 C14H9F3N2
6-amino-8-trifluoromethylphenanthridine
—— (2Z)-3-amino-3-[(4-aminophenyl)sulfanyl]-2-[2-(trifluoromethyl)phenyl]prop-2-enenitrile 305350-87-2 C16H12F3N3S
(2Z)-3-amino-3-[(4-aminophenyl)sulfanyl]-2-[2-(trifluoromethyl)phenyl]prop-2-enenitrile
—— Akt Inhibitor V, Triciribine 35943-35-2 C13H16N6O4
Akt Inhibitor V, Triciribine
—— Velneperit 342577-38-2 C17H24F3N3O3S
Velneperit
—— Panzem NCD 362-07-2 C19H26O3
Panzem NCD
—— Ethyl(2s,3s)-3-[[1-(isopentylcarbamoyl)-3-methyl-butyl]carbamoyl]oxirane-2-carboxylate 88321-09-9 C17H30N2O5
Ethyl(2s,3s)-3-[[1-(isopentylcarbamoyl)-3-methyl-butyl]carbamoyl]oxirane-2-carboxylate
—— 2-(2-Acetamido-4-methylvaleramido)-N-(1-formyl-4-guanidinobutyl)-4-methylvaleramide 24365-47-7 C20H38N6O4
2-(2-Acetamido-4-methylvaleramido)-N-(1-formyl-4-guanidinobutyl)-4-methylvaleramide
—— 6-Bromoindirubin-3'-oxime 667463-62-9 C16H10BrN3O2
6-Bromoindirubin-3'-oxime
—— 2-((4-(1-[11C]methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline 1292799-56-4 C25H20N4O
2-((4-(1-[11C]methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline
—— trans-4-{4-[7-amino-2-(1,2,3-benzothiadiazol-7-yl)-3-chlorofuro[2,3-c]pyridin-4-yl]-1H-pyrazol-1-yl}cyclohexanol 1326712-16-6 C22H19ClN6O2S
trans-4-{4-[7-amino-2-(1,2,3-benzothiadiazol-7-yl)-3-chlorofuro[2,3-c]pyridin-4-yl]-1H-pyrazol-1-yl}cyclohexanol
—— N-[(3S,6S,15S,16R,19S,25R)-25-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]sulfanylmethyl]-3-[[4-(dimethylamino)phenyl]methyl]-12-ethyl-4,16-dimethyl-2,5,11,14,18,21,24-heptaoxo-19-phenyl-17-oxa-1,4,10,13,20-pentazatricyclo[20.4.0.06,10]hexacosan-15-yl]-3-hydroxypyridine-2-carboxamide 120138-50-3 C53H67N9O10S
N-[(3S,6S,15S,16R,19S,25R)-25-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]sulfanylmethyl]-3-[[4-(dimethylamino)phenyl]methyl]-12-ethyl-4,16-dimethyl-2,5,11,14,18,21,24-heptaoxo-19-phenyl-17-oxa-1,4,10,13,20-pentazatricyclo[20.4.0.06,10]hexacosan-15-yl]-3-hydroxypyridine-2-carboxamide
—— 4-Benzyl-1-(beta,4-dihydroxy-alpha-methylphenethyl)piperidinium hydrogen tartrate 23210-58-4 C46H60N2O10
4-Benzyl-1-(beta,4-dihydroxy-alpha-methylphenethyl)piperidinium hydrogen tartrate
—— C646 328968-36-1 C24H19N3O6
C646
—— Rilzabrutinib, (Z)- 1575596-29-0 C36H40FN9O3
Rilzabrutinib, (Z)-
—— Bax channel blocker 335165-68-9 C19H21Br2N3O
Bax channel blocker
—— (4-(5-amino-6-(4-(trifluoromethyl)phenyl)pyrazin-2-yl)-phenyl)(piperazin-1-yl)methanone 1450666-80-4 C22H20F3N5O
(4-(5-amino-6-(4-(trifluoromethyl)phenyl)pyrazin-2-yl)-phenyl)(piperazin-1-yl)methanone