化学品目录 G-化工词典

化学品目录 G

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GSK-2881078
英文名称
GSK-2881078
CAS号
1539314-06-1
分子式
C₁₄H₁₃F₃N₂O₂S
分子量
330.33
中文别名
(R)-1-(1-(甲基磺酰基)丙-2-基)-4-(三氟甲基)-1H-吲哚-5-甲腈; (R)-1-(1-(甲基磺酰基)丙-2-基)-4-(三氟甲基)-1H-吲哚-5-氰基; 化合物GSK2881078; GSK2881078; GSK 2881078; SARM GS2881078; CS-2336; GSK-2881078 (Free base); 1H-Indole-5-carbonitrile, 1-[(1R)-1-methyl-2-(methylsulfonyl)ethyl]-4-(trifluoromethyl)-; 1-[(2R)-1-(Methylsulfonyl)-2-propanyl]-4-(trifluoromethyl)-1H-indole-5-carbonitrile; 1-(1-Methylsulfonylpropan-2-yl)-4-(trifluoromethyl)indole-5-carbonitrile; (R)-1-(1-(methylsulfonyl)propan-2-yl)-4-(trifluoromethyl)-1H-indole-5-carbonitrile; 1-[(2R)-1-methylsulfonylpropan-2-yl]-4-(trifluoromethyl)indole-5-carbonitrile; GSK'078; 1-[(1R)-1-methyl-2-methylsulfonyl-ethyl]-4-(trifluoromethyl)indole-5-carbonitrile; 1-[(2R)-1-methanesulfonylpropan-2-yl]-4-(trifluoromethyl)-1H-indole-5-carbonitrile
用途
靶点为雄激素受体，用于相关医药研究或药物开发。
相关属性
基本信息物化属性
(Z)-2-((2,6-二氯苯基)氨基)-5-(喹喔啉-6-基亚甲基)噻唑-4(5H)-酮
英文名称
GSK-626616
CAS号
1025821-33-3
分子式
C₁₈H₁₀Cl₂N₄OS
分子量
401.27
中文别名
GSK-626616; GSK 626616; GSK626616; 化合物GSK-626616; (5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazolone; 4(5H)-Thiazolone, 2-[(2,6-dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-, (5Z)-; (Z)-2-((2,6-Dichlorophenyl)amino)-5-(quinoxalin-6-ylmethylene)thiazol-4(5H)-one; Gsk-626616; (5Z)-2-(2,6-Dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolone; (5Z)-2-[(2,6-dichlorophenyl)amino]-5-[(quinoxalin-6-yl)methylidene]-4,5-dihydro-1,3-thiazol-4-one; (5Z)-2-((2,6-dichlorophenyl)amino)-5-((quinoxalin-6-yl)methylidene)-4,5-dihydro-1,3-thiazol-4-one; (5Z)-2-(2,6-dichloroanilino)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazol-4-one; (5Z)-2-(2,6-dichloroanilino)-5-(quinoxalin-6-ylmethylene)thiazol-4-one; (5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-1,3-thiazol-4(5H)-one
用途
化学合成；作为有效的口服生物可利用的DYRK3抑制剂，IC50为0.7 nM，可抑制DYRK家族其他成员（如DYRK1A和DYRK2），用于贫血研究，能抑制非刺激和刺激HeLa细胞中S6K1和PRAS40的磷酸化，影响mTORC1活性。
相关属性
基本信息物化属性
3-((6-(4,5-二氢-1H-苯并[d]氮杂庚烷-3(2H)-基)-2-(吡啶-2-基)嘧啶-4-基)氨基)丙酸乙酯盐酸盐
英文名称
GSK-J4 Hydrochloride
CAS号
1797983-09-5
分子式
C₂₄H₂₈ClN₅O₂
分子量
453.96
中文别名
GSK-J4 盐酸盐; N-[2-(2-吡啶基)-6-(1,2,4,5-四氢-3H-3-苯并氮杂-3-基)-4-嘧啶基]-β-丙氨酸乙酯盐酸盐; GSK-J4 HCl; GSK-J4 (hydrochloride); GSK J4 hydrochloride; Ethyl N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-β-alaninate hydrochloride; Ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-yl)amino)propanoate hydrochloride; GSK-J-4 Hydrochloride; β-Alanine, N-[2-(2-pyridinyl)-6-(1,2,4,5-tetrahydro-3H-3-benzazepin-3-yl)-4-pyrimidinyl]-, ethyl ester, hydrochloride (1:1)
用途
生命科学领域；作为细胞渗透性GSK J1前体药物，是选择性H3K27组蛋白去甲基化酶JMJD3和UTX抑制剂，无细胞试验中IC50为60 nM；用于探测H3K27me3去甲基化后果，抑制脂多糖诱导的细胞因子产生及RNA聚合酶II招募；体内研究显示可减轻糖尿病小鼠肾脏疾病发展，降低实验性自身免疫性脑脊髓炎模型疾病严重程度并延迟发病。
相关属性
基本信息物化属性
3-(N-(2-甲氧基-4-(苯氨基)苯基)氨磺酰基)噻吩-2-羧酸甲酯
英文名称
GSK0660
CAS号
1014691-61-2
分子式
C₁₉H₁₈N₂O₅S₂
分子量
418.5
中文别名
GSK0660; 3-[[[2-甲氧基-4-(苯基氨基)苯基]氨基]磺酰基]-2-噻吩羧酸甲酯; GSK 0660; GSK-0660; methyl 3-[(4-anilino-2-methoxy-phenyl)sulfamoyl]thiophene-2-carboxylate; methyl 3-((4-anilino-2-methoxy-phenyl)sulfamoyl)thiophene-2-carboxylate; methyl 3-[(4-anilino-2-methoxyphenyl)sulfamoyl]thiophene-2-carboxylate; methyl 3-(N-(2-methoxy-4-(phenylamino)phenyl)sulfamoyl)thiophene-2-carboxylate; 2-Thiophenecarboxylic acid, 3-[[[2-methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-, methyl ester; 3-[[[2-Methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester; methyl 3-{[2-methoxy-4-(phenylamino)phenyl]sulfamoyl}thiophene-2-carboxylate; Methyl 3-((2-methoxy-4-phenylazanyl-phenyl)sulfamoyl)thiophene-2-carboxylate; Methyl 3-[[[2-methoxy-4-(phenylamino)phenyl]amino]sulfonyl]-2-thiophenecarboxylic acid methyl ester; 3-(2-Methoxy-4-phenylamino-phenylsulfamoyl)-thiophene-2-carboxylic acid methyl ester
用途
化学合成；GSK0660是有效的PPARβ拮抗剂，IC50为155 nM。
相关属性
基本信息物化属性
(2S,5S)-2-(((5-溴吡啶-2-基)氨基)甲基)-5-甲基哌啶-1-基)(3-氟-2-甲氧基苯基)甲酮
英文名称
GSK1059865
CAS号
1191044-58-2
分子式
C₂₀H₂₃BrFN₃O₂
分子量
436.32
中文别名
化合物GSK1059865; 化合物T11477; GSK-1059865; GSK 1059865; ((2S,5S)-2-(((5-Bromopyridin-2-yl)amino)methyl)-5-methylpiperidin-1-yl)(3-fluoro-2-methoxyphenyl)methanone; [(2S,5S)-2-{[(5-Bromo-2-pyridinyl)amino]methyl}-5-methyl-1-piperidinyl](3-fluoro-2-methoxyphenyl)methanone; Methanone, [(2S,5S)-2-[[(5-bromo-2-pyridinyl)amino]methyl]-5-methyl-1-piperidinyl](3-fluoro-2-methoxyphenyl)-; [(2S,5S)-2-[[(5-bromopyridin-2-yl)amino]methyl]-5-methylpiperidin-1-yl]-(3-fluoro-2-methoxyphenyl)methanone; [(2~{S},5~{S})-2-[[(5-bromanylpyridin-2-yl)amino]methyl]-5-methyl-piperidin-1-yl]-(3-fluoranyl-2-methoxy-phenyl)methanone; [(2S,5S)-2-[[(5-bromo-2-pyridyl)amino]methyl]-5-methyl-1-piperidyl]-(3-fluoro-2-methoxy-phenyl)methanone
用途
靶点：Orexin 1 receptor；体内研究：50 and a concomitant decrease of the agonist maximal response. The calculated pKB 50
相关属性
基本信息物化属性
GSK106盐酸盐
英文名称
GSK106 hydrochloride
CAS号
1652591-82-6
分子式
C₂₄H₂₈ClN₅O
分子量
437.97
中文别名
化合物 T24104; GSK-106; GSK 106; 化合物 GSK106; (3-Amino-1-piperidinyl)[2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-benzimidazol-6-yl]-methanone Hydrochloride; GSK106; (3-aminopiperidin-1-yl)-[2-(1-ethylindol-2-yl)-3-methylbenzimidazol-5-yl]methanone;hydrochloride; (3-Aminopiperidin-1-yl)(2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-benzo[d]imidazol-6-yl)methanone hydrochloride; 1-[2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-1,3-benzodiazole-6-carbonyl]piperidin-3-amine hydrochloride; (3-Amino-1-piperidinyl)[2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-benzimidazol-6-yl]methanone hydrochloride (1:1); Methanone, (3-amino-1-piperidinyl)[2-(1-ethyl-1H-indol-2-yl)-1-methyl-1H-benzimidazol-6-yl]-, hydrochloride (1:1)
用途
GSK106 是选择性 PAD4 抑制剂 GSK484 和 GSK199 的非活性对照。
相关属性
基本信息物化属性
GSK121三氟乙酸盐
英文名称
GSK121 trifluoroacetate salt
CAS号
1652591-80-4
分子式
C₂₅H₂₆F₃N₅O₃
分子量
501.5
中文别名
化合物GSK121; (3-Amino-1-piperidinyl)[1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzimidazol-5-yl]methanone trifluoroacetate (1:1); (3-Aminopiperidin-1-yl)(1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzo[d]imidazol-5-yl)methanone trifluoroacetic acid salt; 2,2,2-三氟乙酸与(3-氨基-1-哌啶基)[1-甲基-2-(1-甲基-1H-吲哚-2-基)-1H-苯并咪唑-5-基]甲酮(1:1)化合物; (3-Amino-1-piperidinyl)[1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzimidazol-5-yl]-methanone TFA Salt; GSK121; (3-aminopiperidin-1-yl)-[1-methyl-2-(1-methylindol-2-yl)benzimidazol-5-yl]methanone; (3-Aminopiperidin-1-yl)(1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-benzo[d]imidazol-5-yl)methanone 2,2,2-trifluoroacetate; GSK-121 Trifluoroacetate; 1-[1-methyl-2-(1-methyl-1H-indol-2-yl)-1H-1,3-benzodiazole-5-carbonyl]piperidin-3-amine trifluoroacetic acid; (3-amino-1-piperidyl)-[1-methyl-2-(1-methylindol-2-yl)benzimidazol-5-yl]methanone
用途
GSK-121 Trifluoroacetate 是选择性的 PAD4 抑制剂。
相关属性
基本信息物化属性
GSK163090
英文名称
GSK163090
CAS号
844903-58-8
分子式
C₂₅H₂₉N₅O
分子量
415.53
中文别名
化合物GSK163090; 1-[3-[2-[4-(2-甲基-5-喹啉基)-1-哌嗪基]乙基]苯基]-2-咪唑烷酮; 1-[3-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]phenyl]imidazolidin-2-one; 1-(3-{2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone; 1-[3-[2-[4-(2-Methyl-5-quinolinyl)-1-piperazinyl]ethyl]phenyl]-2-imidazolidinone; 2-Imidazolidinone,1-[3-[2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl]phenyl]-; GSK-163090; GSK 163090; 5-HT1A/B/D receptor antagonist GS163090
用途
化学合成；作为有效的、选择性的和具有口服活性的5-HT1A/1B/1D受体拮抗剂，pKi值分别为9.4/8.5/9.7；抑制血清素再摄取转运蛋白(SerT)的功能活性，pKi值为6.1；具有抗抑郁和抗焦虑活性
相关属性
基本信息物化属性
N-(2,6-二氟苯基)-5-[3-[2-[[5-乙基-2-甲氧基-4-[4-[4-(甲基磺酰基)-1-哌嗪基]-1-哌啶基]苯基]氨基]-4-嘧啶基]咪唑并[1,2-A]吡啶-2-基]-2-甲氧基苯甲酰胺
英文名称
GSK1904529A
CAS号
1089283-49-7
分子式
C₄₄H₄₇F₂N₉O₅S
分子量
851.96
中文别名
IGF-1R和IR抑制剂(GSK1904529A); N-(2,6-二氟苯基)-5-(3-(2-((5-乙基-2-甲氧基-4-(4-(4-(甲基磺酰基)哌嗪-1-基)哌啶-1-基))苯基)氨基)嘧啶-4-基)咪唑并[1,2-A]吡啶-2-基)-2-甲氧基苯甲酰胺; GSK1904529A,IGF-1R / IR酪氨酸激酶抑制剂; 化合物 GSK1904529A; 化合物GSK1904529A; CS-29; GSK-1904529A; GSK 1904529A; GSK 4529; N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl]phenyl]amino]-4-pyrimidinyl]imidazo[1,2-a]pyridin-2-yl]-2-(methyloxy)benzamide; N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)H-imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide; N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide; N-(2,6-Difluorophenyl)-5-(3-{2-[(5-ethyl-2-methoxy-4-{4-[4-(methylsulfonyl)-1-piperazinyl]-1-piperidinyl}phenyl)amino]-4-pyrimidinyl}imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide
用途
靶点 Target Value Insulin Receptor (Cell-free assay) 25 nM IGF-1R (Cell-free assay) 27 nM
相关属性
基本信息物化属性
GSK199 盐酸盐
英文名称
GSK199 hydrochloride
CAS号
1549811-53-1
分子式
C₂₄H₂₉ClN₆O₂
分子量
468.99
中文别名
化合物GSK199; (R)-(3-氨基哌啶-1-基)(2-(1-乙基-1H-吡咯并[2,3-b]吡啶-2-基)-7-甲氧基-1-甲基-1H-苯并[d]咪唑-5-基)甲酮盐酸盐; GSK 199; GSK-199 hydrochloride; GSK-199 Hydrochloric Acid Salt; (R)-(3-Aminopiperidin-1-yl)(2-(1-ethyl-1H-pyrrolo[2,3-b]pyridin-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride
用途
GSK199是一种口服有效的、可逆的、选择性的PAD4抑制剂，可用于类风湿性关节炎的研究。
相关属性
基本信息物化属性
GSK2292767
英文名称
GSK2292767
CAS号
1254036-66-2
分子式
C₂₄H₂₈N₆O₅S
分子量
512.58
中文别名
化合物GSK2292767; REL-N-[5-[4-[5-[[(2R,6S)-2,6-二甲基-4-吗啉基]甲基]-2-恶唑基]-1H-吲唑-6-基]-2-甲氧基-3-吡啶基]甲烷磺酰胺; Gsk2292767; GSK-2292767; AZD 4547; QCR-89; GSK 2292767; PI3Kdelta inhibitor GS2292767; PI3Kδ inhibitor GS2292767; N-{5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-methoxy-3-pyridinyl}methanesulfonamide; N-[5-[4-(5-{[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl}-1,3-oxazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]methanesulfonamide; rel-N-[5-[4-[5-[[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl]-2-oxazolyl]-1H-indazol-6-yl]-2-methoxy-3-pyridinyl]methanesulfonamide; N-[5-[4-[5-[[(2S,6R)-2,6-Dimethylmorpholin-4-yl]methyl]-1,3-oxazol-2-yl]-1H-indazol-6-yl]-2-methoxypyridin-3-yl]methanesulfonamide; N-(5-(4-(5-(((2S,6R)-2,6-dimethylmorpholin-4-yl)methyl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide; N-(5-(4-(5-(((2R,6S)-2,6-Dimethylmorpholino)methyl)oxazol-2-yl)-1H-indazol-6-yl)-2-methoxypyridin-3-yl)methanesulfonamide; N-[5-[4-[5-[[(2R,6S)-2,6-dimethylmorpholin-4-yl]methyl]oxazol-2-yl]-1H-indazol-6-yl]-2-methoxy-3-pyridyl]methanesulfonamide
用途
生命科学，是一种有效和选择性的PI3Kδ的抑制剂，靶点为PI3Kδ。
相关属性
基本信息物化属性
GSK256066三氟乙酸盐
英文名称
GSK256066 Trifluoroacetate
CAS号
1415560-64-3
分子式
C₂₉H₂₇F₃N₄O₇S
分子量
632.61
中文别名
GSK256066 三氟乙酸盐; 化合物T11483; 化合物GSK256066 TRIFLUOROACETATE; 6-((3-(二甲基氨基甲酰基)苯基)磺酰基)-4-((3-甲氧基苯基)氨基)-8-甲基喹啉-3-甲酰胺-2,2,2-三氟乙酸盐; GSK256066 (2,2,2-trifluoroacetic acid); GSK256066 2,2,2-trifluoroacetic acid; GSK256066 (Trifluoroacetate); GSK 256066 Trifluoroacetate; GSK-256066 (2,2,2-trifluoroacetic acid); 6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide 2,2,2-trifluoroacetic acid; 6-((3-(Dimethylcarbamoyl)phenyl)sulfonyl)-4-((3-methoxyphenyl)amino)-8-methylquinoline-3-carboxamide 2,2,2-trifluoroacetate; 6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methyl-quinoline-3-carboxamide Trifluoroacetic acid; 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide 2,2,2-trifluoroacetate (1:1); GSK256066 trifluoroacetate; GSK-256066; GSK 256066; GSK-256066 Trifluoroacetate
用途
生命科学领域，作为选择性、高亲和力的 PDE4 抑制剂，用于慢性阻塞性肺病的研究，抑制 PDE4B 的 IC50 值为 3.2 pM。
相关属性
基本信息物化属性
1-(5-(4-氨基-7-甲基-7H-吡咯并[2,3-d]嘧啶-5-基)-4-氟吲哚啉-1-基)-2-(6-甲基吡啶-2-基)乙酮
英文名称
GSK2656157
CAS号
1337532-29-2
分子式
C₂₃H₂₁FN₆O
分子量
416.45
中文别名
5-[4-氟-1-[(6-甲基-2-吡啶基)乙酰基]-2,3-二氢-1H-吲哚-5-基]-7-甲基-7H-吡咯并[2,3-d]嘧啶-4-胺; PERK抑制剂GSK2656157; GSK2656157抑制剂; 1-(5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethanone; 1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoroindolin-1-yl)-2-(6-methylpyridin-2-yl)ethan-1-one; GSK-2656157; PERK inhibitor GSK2656157; 1-[5-(4-Amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-4-fluoro-2,3-dihydro-1H-indol-1-yl]-2-(6-methyl-2-pyridinyl)ethanone
用途
体外研究（de novo）；作为口服生物有效的PERK选择性抑制剂，其功能不依赖于eIF2α磷酸化，在细胞无细胞实验中对PERK的抑制活性为0.9 nM。
相关属性
基本信息物化属性
N-(3-((2-(4-氨基呋咱-3-基)-1-乙基-1H-咪唑并[4,5-c]吡啶-6-基)氧)苯基)-4-((2-(4-吗啉基)乙基)氧)苯甲酰胺
英文名称
GSK269962A
CAS号
850664-21-0
分子式
C₂₉H₃₀N₈O₅
分子量
570.6
中文别名
GSK269962A; GSK-269962; GSK 269962; ROCK抑制剂GSK269962A; N-[3-[[2-(4-氨基呋咱-3-基)-1-乙基-1H-咪唑并[4,5-c]吡啶-6-基]氧]苯基]-4-[[2-(4-吗啉基)乙基]氧]苯甲酰胺; GSK 269962; GSK269962; GSK-269962; GSK-269962A; N-(3-((2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl)oxy)phenyl)-4-(2-morpholinoethoxy)benzamide; N-(3-{[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy}phenyl)-4-[2-(4-morpholinyl)ethoxy]benzamide; N-[3-[[2-(4-Aminofurazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[[2-(4-morpholinyl)ethyl]oxy]benzamide
用途
化学合成；作为有效的ROCK抑制剂，作用于重组人ROCK1和ROCK2，IC50分别为1.6和4 nM；具有抗炎和血管舒张作用
相关属性
基本信息物化属性
(S)-2-氨基-4-((((2R,3S,4R,5R)-5-(6-氨基-9H-嘌呤-9-基)-3,4-二羟基四氢呋喃-2-基)甲基)(3-(二甲基氨基)丙基)氨基)丁酸 2,2,2-三氟乙酸盐
英文名称
GSK2807 Trifluoroacetate
CAS号
2245255-66-5
分子式
C₂₁H₃₃F₃N₈O₇
分子量
566.53
中文别名
GSK2807三氟乙酸盐; 5'-{[(3S)-3-氨基-3-羧丙基][3-(二甲基氨基)丙基]氨基}-5'-脱氧腺苷三氟乙酸盐(1:1); (S)-2-Amino-4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-(dimethylamino)propyl)amino)butanoic acid 2,2,2-trifluoroacetic acid salt; GSK2807Trifluoroacetate; GSK2807 (Trifluoroacetate); GSK2807; GSK2807 TFA; GSK-2807 Trifluoroacetate; GSK 2807; 5'-{[(3S)-3-Amino-3-carboxypropyl][3-(dimethylamino)propyl]amino}-5'-deoxyadenosine trifluoroacetate (1:1); (2S)-2-amino-4-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methyl-[3-(dimethylamino)propyl]amino]butanoic acid 2,2,2-trifluoroacetic acid
用途
化学合成；作为 SMYD3 有效的、有选择性的 SAM 竞争性抑制剂，用于相关生物活性研究，其 Ki 值为 14 nM，IC50 为 130 nM，对 SMYD2 选择性 24 倍。
相关属性
基本信息物化属性
4-(((3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-((R)-2-((4-氯苄基)(2-(二甲基氨基)乙基)氨基)-1-羟乙基)-1-异丙基-5a,5b,8,8,11a-五甲基-2-氧代-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-十八氢-2H-环戊二烯并[a]苯并菲-9-基)氧基)-2,2-二甲基-4-氧代丁酸
英文名称
GSK2838232
CAS号
1443460-91-0
分子式
C₄₈H₇₃ClN₂O₆
分子量
809.56
中文别名
GSK2838232; HIV-RT抑制剂1; 4-(((3AR,5AR,5BR,7AR,9S,11AR,11BR,13AS)-3A-((R)-2-((4-氯苄基)(2-(二甲氨基)乙基)氨基)-1-羟乙基)-1-异丙基-5A,5B,8,8,11A-五甲基-2-氧代-3,3A,4,5,5A,5B,6,7,7A,8,9,10,11,11A,11B,12,13,13A-十八氢-2H-环戊二烯并[a]苯并菲-9-基)氧基)-2,2-二甲基-4-氧代丁酸; GSK-2838232; GSK-8232; HIV-RT inhibitor 1; 4-[[(3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-[(1R)-2-[(4-chlorophenyl)methyl-[2-(dimethylamino)ethyl]amino]-1-hydroxyethyl]-5a,5b,8,8,11a-pentamethyl-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3H-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid; 28-Norlup-18-en-21-one, 3-(3-carboxy-3-methyl-1-oxobutoxy)-17-((1R)-2-(((4-chlorophenyl)methyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-, (3beta)-; 4-(((3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-((1R)-2-((4-chlorophenyl)methyl-(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-5a,5b,8,8,11a-pentamethyl-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3H-cyclopenta(a)chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid; 4-[[(3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-[(1R)-2-[(4-chlorophenyl)methyl-[2-(dimethylamino)ethyl]amino]-1-hydroxy-ethyl]-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3H-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxo-butanoic acid; 28-Norlup-18-en-21-one, 3-(3-carboxy-3-methyl-1-oxobutoxy)-17-[(1R)-2-[[(4-chlorophenyl)methyl][2-(dimethylamino)ethyl]amino]-1-hydroxyethyl]-, (3b)-; 4-{[(1R,2R,5R,10S,13R,14R, 17S,19R)-5-[(1R)-2- {[(4- chlorophenyl)methyl][2- (dimethylamino)ethyl] amino}-1-hydroxyethyl]- 1,2,14,18,18- pentamethyl-7-oxo-8- (propan-2- yl)pentacyclo[11.8.0.0{circumflex over ()} {2,10}.0{circumflex over ()}{5,9}.0{circumflex over ()}{14,19}] henicos-8-en-17-yl]oxy}- 2,2-dimethyl-4- oxobutanoic acid; 4-{[(3aR,5aR,5bR,7aR,9S,11aR,11bR,13aS)-3a-[(1R)-2-{[(4-chlorophenyl)methyl][2-(dimethylamino)ethyl]amino}-1-hydroxyethyl]-5a,5b,8,8,11a-pentamethyl-2-oxo-1-(propan-2-yl)-2H,3H,3aH,4H,5H,5aH,5bH,6H,7H,7aH,8H,9H,10H,11H,11aH,11bH,12H,13H,13aH-cyclopenta[a]chrysen-9-yl]oxy}-2,2-dimethyl-4-oxobutanoic acid; 4-(((3ar,5ar,5br,9s,11ar,11br,13as)-3a-((r)-2-((4-chlorobenzyl)(2-(dimethylamino)ethyl)amino)-1-hydroxyethyl)-1-isopropyl-5a,5b,8,8,11a-pentamethyl-2-oxo-3,3a,4,5,5a,5b,6,7,7a,8,9,10,11,11a,11b,12,13,13a-octadecahydro-2h-cyclopenta[a]chrysen-9-yl)oxy)-2,2-dimethyl-4-oxobutanoic acid
用途
化学合成。
相关属性
基本信息物化属性
4-((4-((((1R,2S)-2-苯基环丙基)氨基)甲基)哌啶-1-基)甲基)苯甲酸
英文名称
GSK2879552
CAS号
1401966-69-5
分子式
C₂₃H₂₈N₂O₂
分子量
364.48
中文别名
LSD1抑制剂(GSK2879552); 抑制剂GSK2879552; GSK2879552; 4-[[4-[[((1R,2S)-2-Phenylcyclopropyl)amino]methyl]piperidin-1-yl]methyl]benzoic acid; GSK-2879552; GSK 2879552; Benzoic acid, 4-[[4-[[[(1R,2S)-2-phenylcyclopropyl]amino]methyl]-1-piperidinyl]methyl]-; CS-1621
用途
化学合成
相关属性
基本信息物化属性
((3S,4R)-3-氨基-4-羟基哌啶-1-基)(2-(1-(环丙基甲基)-1H-吲哚-2-基)-7-甲氧基-1-甲基-1H-苯并[d]咪唑-5-基)甲酮盐酸盐
英文名称
GSK484 hydrochloride
CAS号
1652591-81-5
分子式
C₂₇H₃₂ClN₅O₃
分子量
510.03
中文别名
GSK484; GSK484盐酸盐; GSK-484盐酸盐; GSK484; GSK484 HCl; ((3S,4R)-3-Amino-4-hydroxypiperidin-1-yl)(2-(1-(cyclopropylmethyl)-1H-indol-2-yl)-7-methoxy-1-methyl-1H-benzo[d]imidazol-5-yl)methanone hydrochloride; Methanone, [(3S,4R)-3-amino-4-hydroxy-1-piperidinyl][2-[1-(cyclopropylmethyl)-1H-indol-2-yl]-7-methoxy-1-methyl-1H-benzimidazol-5-yl]-, hydrochloride (1:1); [(3S,4R)-3-Amino-4-hydroxy-1-piperidinyl]{2-[1-(cyclopropylmethyl)-1H-indol-2-yl]-7-methoxy-1-methyl-1H-benzimidazol-5-yl}methanone hydrochloride (1:1); GSK484 (hydrochloride); PAD4 inhibitor GSK484; PAD4 inhibitor GS484; AOB6992; GTPL8577; [(3S,4R)-3-amino-4-hydroxypiperidin-1-yl]-[2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methylbenzimidazol-5-yl]methanone hydrochloride; (3S,4R)-3-amino-1-{2-[1-(cyclopropylmethyl)-1H-indol-2-yl]-7-methoxy-1-methyl-1H-1,3-benzodiazole-5-carbonyl}piperidin-4-ol hydrochloride; (3S,4R)-3-amino-1-({2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methyl-1,3-benzodiazol-5-yl}carbonyl)piperidin-4-ol hydrochloride; [(3S,4R)-3-amino-4-hydroxy-1-piperidyl]-[2-[1-(cyclopropylmethyl)indol-2-yl]-7-methoxy-1-methyl-benzimidazol-5-yl]methanone hydrochloride
用途
化学合成；作为选择性、可逆的肽基精氨酸脱亚胺酶4 (PAD4)抑制剂，用于体外抑制PAD4瓜氨酸化及体内研究癌症相关肾损伤（如MMTV-PyMT小鼠模型中减少中性粒细胞NETosis和尿蛋白水平）。
相关属性
基本信息物化属性
(Z)-4-(1-(4-(2-(二甲基氨基)乙氧基)苯基)-5-羟基-2-苯基戊-1-烯-1-基)苯酚
英文名称
GSK5182
CAS号
877387-37-6
分子式
C₂₇H₃₁NO₃
分子量
417.54
中文别名
化合物GSK5182; 4-[(1Z)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenylpent-1-en-1-yl]phenol; 4-[(1Z)-1-{4-[2-(Dimethylamino)ethoxy]phenyl}-5-hydroxy-2-phenyl-1-penten-1-yl]phenol; (Z)-4-(1-{4-[2-(DIMETHYLAMINO)ETHOXY]PHENYL}-5-HYDROXY-2-PHENYLPENT-1-ENYL)PHENOL; (Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol; (E/Z)-GSK5182; Benzenebutanol, δ-[[4-[2-(dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]-, (δZ)-; 4-[(Z)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol; GSK-5182; GSK 5182
用途
化学合成;作为4-hydroxytamoxifen类似物，是estrogen-related receptor γ (ERRγ)的特定反向激动剂，可抑制促炎性细胞因子诱导的分解代谢因子
相关属性
基本信息物化属性
(S)-6-(4-(5-(3,5-二氟苯基)-4,5-二氢-1H-吡唑-1-羰基)哌啶-1-基)嘧啶-4-甲腈
英文名称
GSK547
CAS号
2226735-55-1
分子式
C₂₀H₁₈F₂N₆O
分子量
396.39
中文别名
GSK547; 化合物GSK547; (S)-6-(4-(5-(3,5-Difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl)piperidin-1-yl)pyrimidine-4-carbonitrile; 6-[4-[(3S)-3-(3,5-difluorophenyl)-3,4-dihydropyrazole-2-carbonyl]piperidin-1-yl]pyrimidine-4-carbonitrile; GSK'547; GSK-547; RIP1 inhibitor GSK547; RIP1 inhibitor 547; RIP1I; CPD3508; 4-Pyrimidinecarbonitrile, 6-[4-[[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl]carbonyl]-1-piperidinyl]-; 6-{4-[(5S)-5-(3,5-difluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbonyl]piperidin-1-yl}pyrimidine-4-carbonitrile
用途
化学合成；作为高度选择性、有效的RIP1 (RIPK1)抑制剂，在体外可指导骨髓来源巨噬细胞发展成免疫原性表型，上调MHC-II、TNFa和IFNg表达，降低CD206、IL-10和TGFb表达，上调STAT1信号，降低STAT3、STAT5和STAT6信号，增强巨噬细胞抗原捕捉能力；在体内口服给药后24小时浓度稳定且高于L929细胞IC50值，持续给药6周维持高浓度，耐受性良好，可减少原位胰腺导管腺癌小鼠肿瘤负荷并延长生存时间，防止肿瘤和肝转移。
相关属性
基本信息物化属性

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