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Search Results for " topoisomerases "

15

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T32008	GSK299423 GSK-299423,GSK 299423
	GSK299423 (GlaxoSmithKline 299423) is an antibiotic that may have therapeutic effect in patients infected with bacteria expressing New Delhi metal-β-lactamase. Antibiotics inhibit the topoisomerases that the bacteria need to replicate.
T15507	Hycanthone Etrenol(mesylate),Win 249-33,海恩酮	DNA/RNA Synthesis; Topoisomerase; Parasite	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology
	Hycanthone (Etrenol(mesylate)) 是 Lucanthone 的生物活性代谢产物，是一种抗血吸虫病药。它是一个噻吨酮类 DNA 嵌入剂，可抑制 RNA 合成以及 DNA 拓扑异构酶 I 和 II。它通过直接蛋白质结合来抑制核酸生物合成并抑制嘌呤内切核酸酶1，KD 为 10 nM。
T8333	Aurintricarboxylic acid ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056	Apoptosis; P2X Receptor; Influenza Virus; Topoisomerase	Apoptosis; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	Aurintricarboxylic acid (NSC-4056) 是高效的αβ-亚甲基-ATP 敏感选择性P2X1Rs 和P2X3Rs 变构拮抗剂。它是核糖核酸酶和拓扑异构酶 II 的有效抑制剂，可阻止核酸与酶结合。
T2160	Suramin Sodium Salt 苏拉明钠,BAY-205,Suramin hexasodium salt,苏拉明钠盐,NF-060	Apoptosis; Phosphatase; SARS-CoV; Sirtuin; Reverse Transcriptase; Topoisomerase; Parasite	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology
	Suramin Sodium Salt (BAY-205) 是可逆的竞争性蛋白酪氨酸磷酸酶抑制剂。它抑制 IP5K，是抗寄生虫，抗肿瘤和抗血管生成剂。它是sirtuins 的有效抑制剂，也是 SARS-CoV-2 RNA 依赖性 RNA 聚合酶抑制剂。
T27301	Fagaronine chloride NSC157995,NSC 157995,NSC-157995
	Fagaronine chloride is a potent inhibitor of Topoisomerases I.
T39681	Elomotecan hydrochloride BN 80927
	Elomotecan hydrochloride (BN 80927), a camptothecin analog from the homocamptothecin family (hCPT), is a highly potent inhibitor of both topoisomerases I and II. It demonstrates superior efficacy in reducing the proliferation of various tumor cells compared to other reference anticancer drugs targeting these topoisomerases.
T13406L	Zabofloxacin hydrochloride DW-224a	Raf	MAPK
	Zabofloxacin hydrochloride is a potent and seletive bacterial type II and IV topoisomerases inhibitor, has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.
T13406	Zabofloxacin DW-224a Free base	Others	Others
	Zabofloxacin is a potent and seletive bacterial type II and IV topoisomerases inhibitor, and has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia.
T68062	Elomotecan BN 80927 free base
	Elomotecan (BN 80927 free base) 是一种有效的拓扑异构酶 I (topoisomerases I) 和 II 抑制剂。Elomotecan 是属于高喜树碱家族 (hCPT) 的喜树碱类似物。与其他拓扑异构酶 I 和 II 的参考抗癌药物相比，Elomotecan 减少不同肿瘤细胞的增殖效果更好。
T11289	Finafloxacin	Others	Others
	Finafloxacin, a fluoroquinolone antimicrobial agent from a new 8-cyano subclass, is most effective in slightly acidic environments (pH 5.0-6.0), a condition where other fluoroquinolones typically reduce in activity. It selectively targets bacterial type II topoisomerases, such as DNA gyrase and DNA topoisomerase IV, making it suitable for treating serious bacterial infections particularly in acidic contexts, including urinary tract infections (UTIs) and Helicobacter pylori infections.
T36485	Becatecarin
	Becatecarin is a water-soluble, diethylaminoethyl analog of the antineoplastic antibiotic rebeccamycin. It intercalates into DNA, stabilizing the DNA-topoisomerase complex. This results in the potent catalytic inhibition of both topoisomerases I and II, initiating DNA cleavage and apoptosis. Becatecarin, alone or in combination with other compounds, has anti-cancer as well as myelosuppressive effects in vivo. It is also a transport substrate of the ATP-binding cassette (ABC) transporter ABCG2.
T63070	EGFR-IN-45
	EGFR-IN-45 是一种有效的表皮生长因子受体 (EGFR) 泛抑制剂，能够作用于 EGFR (IC50: 0.4 μM) 和 CDK2 (IC50: 1.6 μM)。EGFR-IN-45 对拓扑异构酶 Topo I 和 Topo II 也具有抑制作用。EGFR-IN-45 能将癌细胞的细胞周期阻滞在 G1 前期，并诱导细胞凋亡 (apoptosis)。
T36889	Methyl alpha-eleostearate
	Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supple...
T36888	9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester
	9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPA...
T36698	9(Z),11(E),13(E)-Octadecatrienoic Acid
	9(Z),11(E),13(E)-Octadecatrienoic Acid (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1...

化合物

Cat.No: T32008

Synonym: GSK-299423,GSK 299423

Cat.No: T15507

Synonym: Etrenol(mesylate),Win 249-33,海恩酮

Target: DNA/RNA Synthesis, Topoisomerase, Parasite

Aurintricarboxylic acid

Cat.No: T8333

Synonym: ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056

Target: Apoptosis, P2X Receptor, Influenza Virus, Topoisomerase

Suramin Sodium Salt

Cat.No: T2160

Synonym: 苏拉明钠,BAY-205,Suramin hexasodium salt,苏拉明钠盐,NF-060

Target: Apoptosis, Phosphatase, SARS-CoV, Sirtuin, Reverse Transcriptase, Topoisomerase, Parasite

Fagaronine chloride

Cat.No: T27301

Synonym: NSC157995,NSC 157995,NSC-157995

Elomotecan hydrochloride

Cat.No: T39681

Synonym: BN 80927

Zabofloxacin hydrochloride

Cat.No: T13406L

Synonym: DW-224a

Target: Raf

Cat.No: T13406

Synonym: DW-224a Free base

Target: Others

Cat.No: T68062

Synonym: BN 80927 free base

Cat.No: T11289

Target: Others

Cat.No: T36485

Cat.No: T63070

Methyl alpha-eleostearate

Cat.No: T36889

9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester

Cat.No: T36888

9(Z),11(E),13(E)-Octadecatrienoic Acid

Cat.No: T36698

Cat. No.	Product Name	Target	Signaling Pathways
T21065	Artemisitene	Others	Others
	Artemisitene 是青蒿素的氧化形式，是一种抗疟药。青蒿素前体是青蒿素生物合成的重要基础物质，包括青蒿素 B、青蒿素、青蒿酸等。
T5784	Topotecan NSC 609669,拓扑替康,SKF 104864A	Topoisomerase; Autophagy	Autophagy; DNA Damage/DNA Repair
	Topotecan (NSC-609669) 是一种拓扑异构酶 I 抑制剂，通过抑制 DNA 拓扑异构酶起抗肿瘤作用，可用于治疗卵巢癌。
T1737	Genistein NPI 031L,三叶草,染料木素,金雀异黄酮	Apoptosis; EGFR; Endogenous Metabolite; Autophagy	Angiogenesis; Apoptosis; Autophagy; JAK/STAT signaling; Metabolism; Tyrosine Kinase/Adaptors
	Genistein (NPI 031L) 是一种大豆异黄酮，是一种多重的酪氨酸激酶抑制剂，通过改变细胞凋亡，细胞周期和血管生成以及抑制转移对多种癌症有化疗作用。
T2S1792	Lycobetaine 石蒜内胺,Ungeremine,石蒜醋胺,石蒜碱内铵盐	Antibacterial	Microbiology/Virology
	Lycobetaine (Ungeremine) 是一种潜在的抗罗克福尔青霉和黑曲霉的生物杀菌剂。它对柱状黄杆菌有很强的抗菌活性。它有效地靶向哺乳动物以及细菌I 型和II 型拓扑异构酶。它显示出强烈的乙酰胆碱酯酶抑制活性（IC(50) 值为 0.35 microM）。它具有抗原生动物活性，在体外试验中对Trypanosoma brucei rhodesiense、T. cruzi 表现出良好的活性。
TN1169	1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-β-D-glucopyranoside 1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-beta-glucopyranoside	Topoisomerase	DNA Damage/DNA Repair
	1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-beta-glucopyranoside may have DNA topoisomerases I and II inhibitory activity and cytotoxicity.
TN4107	Ganoderic acid X	ERK; Mdm2; MAPK; Caspase; Topoisomerase; JNK; p53	Apoptosis; DNA Damage/DNA Repair; MAPK; Proteases/Proteasome
	Ganoderic acid X is a potential Mdm2 inhibitor(K(i) = 16nM). It is a potential anticancer drug, inhibits topoisomerases and induces apoptosis of cancer cells.
TMA1012	Ganoderiol F	Androgen Receptor; HIV Protease; Autophagy	Autophagy; Endocrinology/Hormones; Microbiology/Virology; Proteases/Proteasome
	Ganoderiol F has anti-inflammatory, cytotoxic and anti-HIV activity, it inhibits activity of topoisomerases in vitro, and it inhibits human immunodeficiency virus-1 protease with IC(50) values of 20-40 microM. It induced HO-1 expression, activation of the mitogen-activated protein kinase EKR and up-regulation of cyclin-dependent kinase inhibitor p16 and suppressed lipopolysaccharide (LPS)-induced nitric oxide (NO) production.

天然产物

Cat.No: T21065

Target: Others

Cat.No: T5784

Synonym: NSC 609669,拓扑替康,SKF 104864A

Target: Topoisomerase, Autophagy

Cat.No: T1737

Synonym: NPI 031L,三叶草,染料木素,金雀异黄酮

Target: Apoptosis, EGFR, Endogenous Metabolite, Autophagy

Cat.No: T2S1792

Synonym: 石蒜内胺,Ungeremine,石蒜醋胺,石蒜碱内铵盐

Target: Antibacterial

1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-β-D-glucopyranoside

Cat.No: TN1169

Synonym: 1,4-Dihydroxy-2-carbomethoxy-3-prenylnaphthalene-1-O-beta-glucopyranoside

Target: Topoisomerase

Ganoderic acid X

Cat.No: TN4107

Target: ERK, Mdm2, MAPK, Caspase, Topoisomerase, JNK, p53

Cat.No: TMA1012

Target: Androgen Receptor, HIV Protease, Autophagy

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