“Tutalthromycin second gen”的搜索结果
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Dehydrogenase 抑制剂
Ammonium Glycyrrhizinate是来自Licorice root的一种独特产品,具有极高的甜味。
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COX-1 抑制剂
Ibuprofen (Advil)是一种非甾体抗炎药(NSAID),靶向COX-1,IC50为13 μM。
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- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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DNA Methyltransferase 抑制剂
Decitabine是一种次甲基化剂,它通过抑制DNA甲基转移酶来使DNA次甲基化。
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- Borbala Szabo, .et al. Aspirin mediates its antitumoral effect through inhibiting PTTG1 in pituitary adenoma, J Clin Endocrinol Metab, 2022, Sep 5;dgac496 PMID: 36059148
- Sangni Qian, .et al. Hypermethylation of tumor suppressor lncRNA MEF2C-AS1 frequently happened in patients at all stages of colorectal carcinogenesis, Clin Epigenetics, 2022, Sep 5;14(1):111 PMID: 36064442
- Borb??la Szab??, .et al. Demethylation status of somatic DNA extracted from pituitary neuroendocrine tumors indicates proliferative behavior, J Clin Endocrinol Metab, 2020, Jun 1;105(6):dgaa156 PMID: 32232382
- Bracha Shraibman, .et al. Human Leukocyte Antigen (HLA) Peptides Derived from Tumor Antigens Induced by Inhibition of DNA Methylation for Development of Drug-facilitated Immunotherapy, Mol Cell Proteomics, 2016, Sep; 15(9): 3058-3070 PMID: 27412690
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NLRP3 inflammasome 抑制剂
Isoliquiritigenin是从光果甘草根中分到的黄酮类化合物,具有抗肿瘤的活性。目前正处于试验阶段,用于癌症和可卡因成瘾的辅助治疗的研究。
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Protein kinase 抑制剂
Apigenin是中央苯并二氮杂central受体的配体,其Ki为4μM竞争性抑制氟硝西epa的结合,发挥抗焦虑和轻微的镇静作用。
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Lipoxygenase 抑制剂
Baicalein是一种类黄酮,最初从黄cut的根中分离出来。Baicalein抑制脂质过氧化 (通过TBARS的产生评估),IC50值为5 ?M。
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Antibacterial agent
Retapamulin (SB-275833)是一种抗菌剂,特别是蛋白质合成抑制剂。
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- Merianne Mohamad, .et al. Sal-type ABC-F proteins: intrinsic and common mediators of pleuromutilin resistance by target protection in staphylococci, Nucleic Acids Res, 2022, Feb 28;50(4):2128-2142 PMID: 35137182
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dehydrogenase inhibitor
Gossypol是一种多酚醛,渗透细胞并作为几种脱氢酶的抑制剂。
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- Amy L. Farthing, .et al. Response of northern bobwhites fed single doses of gossypol, Wildlife Society Bulletin, 2018, 42(3):460-466;
- Jin Qu, .et al. Gossypol potentiates carboplatin effects against ovarian cancer, Biomed Res, 2017, 28 (8): 3355-3361
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Dehydrogenase 抑制剂
Leflunomide是一种嘧啶合成抑制剂,属于DMARD类药物。来氟米特用于缓解类风湿性关节炎引起的症状,如炎症、肿胀、僵硬和关节痛。
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Procollagen C-proteinase 抑制剂
UK-383367是一种前胶原C蛋白酶抑制剂,IC50为44 nM,对MMP具有优异的选择性。
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Hydrogen peroxide 抑制剂
Acetanilide在过氧化氢中用作抑制剂,并用于稳定纤维素酯清漆。
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Dehydrogenase 抑制剂
CPI-613是合成的α-硫辛酸硫辛酸类似物的对映异构体的外消旋混合物,具有潜在的化学预防和抗肿瘤活性。
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- Takuji Sakuratani, .et al. Downregulation of ARID1A in gastric cancer cells: a putative protective molecular mechanism against the Harakiri-mediated apoptosis pathway, Virchows Arch, 2020, Aug 13 PMID: 32789692
- Egawa Y, .et al. Therapeutic potential of CPI-613 for targeting tumorous mitochondrial energy metabolism and inhibiting autophagy in clear cell sarcoma, PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
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Androgen Receptor 抑制剂
Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂,IC50 为 16 nM。ARN-509与靶组织中的AR结合,从而阻止了雄激素诱导的受体激活,并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。
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- Frédérique Mittler, .et al. High-Content Monitoring of Drug Effects in a 3D Spheroid Model, Front Oncol, 2017, 7: 293 PMID: 29322028
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Dihydroorotate Dehydrogenase 抑制剂
Brequinar是二氢乳清酸脱氢酶的抑制剂,二氢乳清酸脱氢酶是从头进行嘧啶生物合成的酶。
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rRNA biogenesis 抑制剂
Quarfloxin (CX-3543)是一种具有抗肿瘤活性的氟喹诺酮衍生物。quarfloxin破坏核蛋白和核糖体dna (rdna)模板中g-四链体dna结构之间的相互作用,这是在癌细胞中过度表达的rrna生物发生的关键相互作用;这种g-四链体dna的破坏:异常rrna生物发生中的蛋白质相互作用可能导致核糖体合成和肿瘤细胞凋亡的抑制。
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- Janne J. M. van Schie, .et al. Warsaw Breakage Syndrome associated DDX11 helicase resolves G-quadruplex structures to support sister chromatid cohesion, Nat Commun, 2020, 11: 4287 PMID: 32855419
- Yue Sheng, .et al. Role of c-Myc haploinsufficiency in the maintenance of HSCs, Blood, 2020, Aug 21 PMID: 32822452
- Hald øH, .et al. Inhibitors of ribosome biogenesis repress the growth of MYCN-amplified neuroblastoma, Oncogene, 2018, Dec 12 PMID: 30542116
- Louise E. Kerry, .et al. Selective inhibition of RNA polymerase I transcription as a potential approach to treat African trypanosomiasis, PLoS Negl Trop Dis, 2017, Mar; 11(3): e0005432 PMID: 28263991
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COX/5-LOX 抑制剂
Tepoxalin是花生四烯酸代谢的双重环氧合酶/5-脂氧合酶抑制剂,具有有效的抗炎活性和良好的胃肠道功能。
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topoisomerase 1 抑制剂
GENZ-644282是拓扑异构酶I的非喜树碱抑制剂,具有潜在的抗肿瘤活性。
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Lck 抑制剂
AMG-47a是口服有效的Lck和T细胞增殖抑制剂。它在抗CD3诱导的小鼠IL-2产生中表现出抗炎活性(ED50 11 mg/kg)。
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Smad 抑制剂
Kartogenin能有效诱导人骨髓间充质干细胞分化为软骨细胞。
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CYP17A1/androgen synthesis 抑制剂
TAK-700 Salt (Orteronel Salt)是一种雄激素合成抑制剂。它选择性地抑制在睾丸,肾上腺和前列腺肿瘤组织中表达的酶CYP17A。
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2OG oxygenases 抑制剂
IOX1是2OG加氧酶(包括JmjC脱甲基酶)的有效且广谱抑制剂。
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AChE 抑制剂
Desoxypeganine hydrochloride是一种AChE(乙酰胆碱酯酶)抑制剂,已用于治疗阿尔茨海默氏痴呆症。
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FLAP 抑制剂
AZD6642是5-Lipoxygenase激活蛋白(FLAP)的抑制剂,可用于治疗炎症。
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Collagen proline hydroxylase 抑制剂
Collagen proline hydroxylase抑制剂是胶原脯氨酸羟化酶抑制剂。
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5-lipoxygenase 抑制剂
Esculetin是一种酚类化合物,可作为5-LO(5-脂氧合酶,5-LOX)抑制剂。
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FLAP 抑制剂
MK591是5-Lipoxygenase激活蛋白(FLAP)的选择性和特异性抑制剂。
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TAK1/MAP4K2 抑制剂
NG25和TAK1抑制TLR7和TLR9激动剂激活IKK,并阻止Gen2.2细胞中这些配体诱导的1型IFN分泌。
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lipoxygenase 抑制剂
Nordihydroguaiaretic acid是从杂酚丛生的Larrea divaricata中分离出来的天然酚类化合物,在体外和体内均具有抗肿瘤活性。其类似物正在临床开发中,用于难治性实体瘤。
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Glucocerebroside synthase 抑制剂
Eliglustat tartrate通常用作酒石酸盐,据信Eliglustat通过抑制葡萄糖基神经酰胺合酶起作用。
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- Zunke F, .et al. Reversible Conformational Conversion of α-Synuclein into Toxic Assemblies by Glucosylceramide, Neuron, 2018, Jan 3;97(1):92-107.e10 PMID: 29290548
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GL1 synthase 抑制剂
Genz-123346 free base是GL1合酶的抑制剂,可阻止神经酰胺向GL1的转化。抑制GM1的IC50为14 nM。
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Glucosylceramide synthase 抑制剂
Eliglustat是葡萄糖神经酰胺合成酶的一种特异而有效的抑制剂。
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Ferroptosis inhibitor
RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
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- Sampilvanjil A, .et al. Cigarette smoke extract induces ferroptosis in vascular smooth muscle cells, Am J Physiol Heart Circ Physiol, 2020, Mar 1;318(3):H508-H518 PMID: 31975626
- Fujiki K, .et al. Blockade of ALK4/5 signaling suppresses cadmium- and erastin-induced cell death in renal proximal tubular epithelial cells via distinct signaling mechanisms, Cell Death Differ, 2019, Feb 25 PMID: 30804470
- Samantha W. Alvarez, .et al. NFS1 undergoes positive selection in lung tumours and protects cells from ferroptosis, Nature, 2017, Nov 30; 551(7682): 639-643 PMID: 29168506
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Dehydrogenase 抑制剂
AG-120是1型异柠檬酸脱氢酶(IDH1)的抑制剂,具有潜在的抗肿瘤活性。
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alcohol dehydrogenase 抑制剂
Fomepizole是一种醇脱氢酶抑制剂,用于治疗成年人的乙二醇和甲醇中毒。
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Fibrillogenesis 抑制剂
Eprodisate Sodium是Eprodisate的口服二钠盐形式,Eprodisate是一种带负电的原纤维化磺化抑制剂,可用于治疗淀粉样蛋白A(AA)淀粉样变性。
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KDM 抑制剂
2,4-Pyridinedicarboxylic Acid是针对JMJD2A(KDM4A),KDM4C,KDM4E(IC50、1.4μM),KDM5B(IC50、3μM),KDM6A和 其他的2-氧合酶。
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BRAF 抑制剂
Lifirafenib (BGB-283),也称为Beigene-283,在生化分析中有效抑制RAF家族激酶和EGFR活性,重组BRAFV600E激酶结构域,EGFR和EGFR T790M/L858R突变体的IC50值为23、29和495 nM。
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COX and lipo-oxygenase 抑制剂
Timegadine被发现是一种有效的竞争性环加氧酶(COX)和脂加氧酶抑制剂,IC50的范围从5 nM(洗兔血小板)到20μM(大鼠脑)。在马血小板匀浆的细胞溶质级分和洗涤过的兔血小板中,脂氧化酶的浓度为100μM和100μM。
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Antispasmodic Agent
Pitofenone Hydrochloride是抗痉化合物。它是乙酰胆碱酯酶活性的有效抑制剂。
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12-Lipoxygenase (12-LOX) inhibitor
ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
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COX 抑制剂
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
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CYP2C9 inhibitor
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.
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D2DR and D4DR inhibitor
Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.
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CA9 inhibitor
Benzthiazide is a long-acting diuretic and a hypertension agent. Benzthiazide is an inhibitor of carbonic anhydrase 9 (CA9), with Kis of 8.0, 8.8 and 10 nM for CA9, CA2 and CA1, respectively. Benzthiazide also suppresses proliferation of cancer cells.
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MMP inhibitor
Iincyclinide, also known as CMT-3 and COL-3, is a MMP inhibitor and a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.
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MCL-1 Inhibitor
VU661013 is a MCL-1 Inhibitor Combined with Venetoclax Rescues Venetoclax Resistant Acute Myelogenous Leukemia.
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TYROSINE 3-MONOOXYGENASE inhibitor
Metyrosine is an inhibitor of the enzyme TYROSINE 3-MONOOXYGENASE.
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MAPKAPK5 inhibitor
GLPG-0259 is a small-molecule inhibitor of mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5), a kinase enzyme that plays a role in important inflammatory pathways
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Microtubule/Tubulin Inhibitor
SSE15206 is a pyrazolinethioamide derivative that has potent antiproliferative activities in cancer cell lines of different origins and overcomes resistance to microtubule-targeting agents.
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COX-2 抑制剂
Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
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