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22

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T19654 Guanoclor

胍氯酚,VATENSOL

Others Others
Guanoclor (VATENSOL) 也称为guanochlor,是一种交感神经药物。已知它与猪肾膜中的非肾上腺素能位点结合。
T13383 Zamicastat

BIA 5-1058

BCRP; Hydroxylase; P-gp Membrane transporter/Ion channel; Metabolism; Neuroscience
Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂,可透过血脑屏障引起中枢和周边效应,具有降血压作用。它也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂,IC50值分别为 73.8 和 17.0 μM。
T7877 Thiacetazone

氨硫脲,Diazam,Thioacetazone,Neustab,Neotibil

Others; Antibacterial; Antibiotic Microbiology/Virology; Others
Thiacetazone (Diazam) 是一种氨基硫脲抗结核剂,也是一种具有口服活性抗生素。它具有抗菌作用,可抑制结核分枝杆菌 H37Rv 的生长,MIC 值为 0.1 μg/mL。
T6604 Nepicastat hydrochloride

Nepicastat HCl,内匹司他盐酸盐,RS-25560-197 hydrochloride,SYN-117 hydrochloride,Nepicastat (SYN-117) HCl

Hydroxylase Metabolism
Nepicastat hydrochloride (RS-25560-197 hydrochloride) 是一种选择性的,有效的,口服活性的多巴胺 β 羟化酶(dopamine-beta-hydroxylase)抑制剂,对牛和人多巴胺 β 羟化酶的IC50分别为IC50=8.5 nM 和IC50=9 nM。Nepicastat HCl 可以穿过血脑屏障。
T20373 1-Phenylpyrrole

NSC16581,NSC-16581,1-苯基吡咯,NSC 16581

Others Others
1-Phenylpyrrole (NSC-16581) 可抑制大鼠肝脏微粒体中 CYP450 依赖性单加氧酶活性。
T20700 Racemetirosine

Others Others
Racemetirosine 是一种酪氨酸 3-单加氧酶抑制剂,因此会抑制儿茶酚胺的合成。
T0293 Metyrapone

美替拉酮,甲吡酮,NSC-25265,Su-4885

Others; P450; Dehydrogenase; Autophagy Autophagy; Metabolism; Others
Metyrapone (NSC-25265) 是 STEROID 11-BETA-MONOOXYGENASE 酶抑制剂。 它被用作库欣综合征诊断中下丘脑-垂体反馈机制的测试。
TP1344 Luciferase

Others Others
Luciferase 是一种在生物发光细菌中发现的依赖黄素的单加氧酶。 Luciferase 是识别和表征功能变体的宝贵工具,可用于研究基因表达、细胞内信号传导、转录因子、受体活性和蛋白质折叠。
T28202 NSC-152035

Racemetirosine methyl ester HCl,NSC 152035,Racemetirosine methyl ester hydrochloride

NSC-152035 is an inhibitor of tyrosine 3-monooxygenase.
T13258 UPF-648 sodium salt

Others Others
UPF-648 sodium salt is an inhibitor of kynurenine 3-monooxygenase (KMO) and exhibits highly active at 1 uM (81 ± 10% KMO inhibition).
T32743 Licodione

Licodione is a Cytochrome P450 Monooxygenase Catalyzing 2-Hydroxylation of 5-Deoxyflavanone.
T70041 GSK065

GSK065 is a potent inhibitor of kynurenine-3-monooxygenase (KMO).
T0293L Metyrapone Tartrate

SU 4885,Metopirone tartrate,SU-4885,SU4885

Metyrapone Tartrate is an inhibitor of the STEROID 11-beta-monooxygenase enzyme which is used as a test for feedback hypothalamic-pituitary mechanism in the diagnosis of Cushing SYNDROME.
T15426 GSK180

Hydroxylase Metabolism
GSK180 is a selective competitive inhibitor of kynurenine 3-monooxygenase (KMO; IC50: ~6 nM), an enzyme involved in tryptophan metabolism.
T11470 GSK 366

Hydroxylase Metabolism
GSK 366 is a potent kynurenine-3-monooxygenase (KMO) inhibitor (IC50s: 0.7 nM and 2.3 nM for P. fluorescens-KMO and human KMO).
T13258L UPF-648

Others Others
UPF-648 is a potent kynurenine 3-monooxygenase inhibitor. It also shows highly active at 1 uM (81 ± 10% KMO inhibition).
T63613 JM6

JM6 是弱犬尿氨酸 3-单加氧酶 (kynurenine 3-monooxygenase, KMO) 抑制剂,能够作用于小鼠 KMO (IC50: 19.85 μM)。JM6 能够用于研究阿尔茨海默病。
T80635 Gentisuric acid

Drug Metabolite Metabolism
Gentisuric Acid,作为Aspirin的代谢产物同时也是α-酰胺化单加氧酶(PAM)的底物,可抵御Mitomycin C导致的DNA损伤。
T37659 5-hydroxy Omeprazole

5-hydroxy Omeprazole is a major metabolite of omeprazole , an inhibitor of the gastric H+/K+-ATPase pump.[1] 5-hydroxy Omeprazole is produced from omeprazole by the action of cytochrome P450 (CYP) isoform 2C19, a monooxygenase. [2][3] CYP2C19 polymorphisms significantly influence the metabolism of omeprazole, and individuals may be classified as homozygous extensive metabolizers, heterozygous extensive metabolizers, and poor metabolizers.[1]
T82190 H-Met-Val-OH

H-Met-Val-OH是一种游离N端蛋氨酸的二肽。该化合物对cDNA表达的FMO1和FMO3表现活性,并可能在神经突起生长中有应用。
T13460 (+)-Cevimeline hydrochloride hemihydrate

(+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011

Others Others
(+)-Cevimeline hydrochloride hemihydrate ((+)-SNI-2011) 是一种有效的 mAChR 激动剂。
T13421 (-)-Cevimeline hydrochloride hemihydrate

(-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate

ALK Angiogenesis; Tyrosine Kinase/Adaptors
(-)-Cevimeline hydrochloride hemihydrate ((-)-SNI-2011) 是一种新型mAChR 激动剂,是一种治疗干燥综合征口干症的候选治疗药物。

化合物

Guanoclor
Cat.No: T19654
Synonym: 胍氯酚,VATENSOL
Target: Others
Zamicastat
Cat.No: T13383
Synonym: BIA 5-1058
Target: BCRP, Hydroxylase, P-gp
Thiacetazone
Cat.No: T7877
Synonym: 氨硫脲,Diazam,Thioacetazone,Neustab,Neotibil
Target: Others, Antibacterial, Antibiotic
Nepicastat hydrochloride
Cat.No: T6604
Synonym: Nepicastat HCl,内匹司他盐酸盐,RS-25560-197 hydrochloride,SYN-117 hydrochloride,Nepicastat (SYN-117) HCl
Target: Hydroxylase
1-Phenylpyrrole
Cat.No: T20373
Synonym: NSC16581,NSC-16581,1-苯基吡咯,NSC 16581
Target: Others
Racemetirosine
Cat.No: T20700
Synonym:
Target: Others
Metyrapone
Cat.No: T0293
Synonym: 美替拉酮,甲吡酮,NSC-25265,Su-4885
Target: Others, P450, Dehydrogenase, Autophagy
Luciferase
Cat.No: TP1344
Synonym:
Target: Others
NSC-152035
Cat.No: T28202
Synonym: Racemetirosine methyl ester HCl,NSC 152035,Racemetirosine methyl ester hydrochloride
Target:
UPF-648 sodium salt
Cat.No: T13258
Synonym:
Target: Others
Licodione
Cat.No: T32743
Synonym:
Target:
GSK065
Cat.No: T70041
Synonym:
Target:
Metyrapone Tartrate
Cat.No: T0293L
Synonym: SU 4885,Metopirone tartrate,SU-4885,SU4885
Target:
GSK180
Cat.No: T15426
Synonym:
Target: Hydroxylase
GSK 366
Cat.No: T11470
Synonym:
Target: Hydroxylase
UPF-648
Cat.No: T13258L
Synonym:
Target: Others
JM6
Cat.No: T63613
Synonym:
Target:
Gentisuric acid
Cat.No: T80635
Synonym:
Target: Drug Metabolite
5-hydroxy Omeprazole
Cat.No: T37659
Synonym:
Target:
H-Met-Val-OH
Cat.No: T82190
Synonym:
Target:
(+)-Cevimeline hydrochloride hemihydrate
Cat.No: T13460
Synonym: (+)-AF102B hydrochloride hemihydrate,(+)-SNI-2011
Target: Others
(-)-Cevimeline hydrochloride hemihydrate
Cat.No: T13421
Synonym: (-)-SNI-2011,(-)-AF102B hydrochloride hemihydrate
Target: ALK
Cat. No. Product Name Target Signaling Pathways
TN1576 Diallyl disulfide

IL Receptor; NOS; NF-κB Immunology/Inflammation; NF-κB
Diallyl disulfide 能够抑制人角鲨烯单加氧酶,抑制角鲨烯环氧化的 IC50为 400 μM。它也具有抗肿瘤作用,同miR-200b 和miR-22联合使用可增强该作用。
T6S0923 Hypericin

Hypericine,金丝桃素,Cyclosan

Apoptosis; Antiviral; Influenza Virus; Tyrosine Kinases; Antibacterial; PKC Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Microbiology/Virology; Tyrosine Kinase/Adaptors
Hypericin (Cyclosan) 是贯叶连翘的提取物,有抗菌、抗病毒、抗肿瘤和抗抑郁作用。
T4829 3-Hydroxyphenylacetic acid

Others; Endogenous Metabolite Metabolism; Others
3-Hydroxyphenylacetic acid 是内源性代谢产物的一种。
T11680 Isoasatone A

P450 Metabolism
Isoasatone A 是一种具有抗虫作用的天然产物,分离自Heterotropa takaoiM。它作用于细胞色素 P450 单加氧酶和谷胱甘肽转移酶,产生抗S. litura 作用。
TN1078 Seneciphylline

千里光菲灵碱,千里光非灵

P450; GST Metabolism; oxidation-reduction
Seneciphylline 是一种有毒的吡咯烷核生物碱,存在于千里光植物中。它显著增加了环氧水合酶和谷胱甘肽-S-转移酶的特性,但导致细胞色素 P-450 和相关单加氧酶特性的抑制。
T78483 Benzydamine N-Oxide

Benzydamine N-Oxide,作为Benzydamine的代谢产物,主要用于测定含黄素单加氧酶(flavin-containing monooxygenase)的活性。
T80656 Cannflavin A

Cannflavin A,源自大麻(Cannabis sativa L),具备抗癌、神经保护及抗炎活性。该化合物有效抑制Aβ1-42的聚集,并阻断犬尿氨酸-3-单加氧酶(KMO)的活性,进而通过caspase-3裂解途径激活细胞凋亡(apoptosis)。

天然产物

Diallyl disulfide
Cat.No: TN1576
Synonym:
Target: IL Receptor, NOS, NF-κB
Hypericin
Cat.No: T6S0923
Synonym: Hypericine,金丝桃素,Cyclosan
Target: Apoptosis, Antiviral, Influenza Virus, Tyrosine Kinases, Antibacterial, PKC
3-Hydroxyphenylacetic acid
Cat.No: T4829
Synonym:
Target: Others, Endogenous Metabolite
Isoasatone A
Cat.No: T11680
Synonym:
Target: P450
Seneciphylline
Cat.No: TN1078
Synonym: 千里光菲灵碱,千里光非灵
Target: P450, GST
Benzydamine N-Oxide
Cat.No: T78483
Synonym:
Target:
Cannflavin A
Cat.No: T80656
Synonym:
Target:
TargetMol Loading
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