“Tutalthromycin second gen”的搜索结果
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CYP3A4/5 inhibitor and substrate
Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
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CYP17 lyase inhibitor
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
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CYP450 dependent inhibitor
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).
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PDE7/GSK3 inhibitor
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively.
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LXR agonist
RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
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IDH inhibitor
Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
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IDO-1 inhibitor
IDO-IN-4 is an indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor, extracted from patent WO2014150677A1, Compound example 1 enantiomer 1.
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IDO inhibitor
IDO-IN-5 (NLG-1489) is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO WO2012142237A1, compound 1489, has an IC50 of 1-10 μM.
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IDO inhibitor
IDO-IN-3 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor with an IC50 of 290 nM.
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PDE-9 inhibitor
PDE-9 inhibitor is useful for neurodegenerative diseases.
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AhR agonist
ITE is a potent endogenous agonist of aryl hydrocarbon receptor (AhR), binding directly to AHR, with a Ki of 3 nM. ITE also has immunosuppressive activity.
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hIDO2 inhibitor
GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.
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IDO inhibitor
IDO-IN-12 is an indoleamine 2,3-dioxygenase (IDO) inhibitor extracted from patent WO 2017181849 A1.
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NAMPT activator
SBI-797812 is a novel NAMPT activator, elevating liver NAD+, turning NAMPT into a "super catalyst" that more efficiently generates NMN.
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IDH1 inhibitor
Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ?? 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells.
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dual PDE7/GSK-3 inhibitor
VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
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IDO/TDO dual inhibitor
IDO/TDO-IN-1 is a highly potent and orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50s of 9.7 and 47 nM, respectively .
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Hsp47 inhibitor
Col003 is a potent inhibitor of Hsp47, competitively binds to the collagen binding site on Hsp47 (IC50, 1.8 μM), and inhibits collagen secretion by destabilizing the collagen triple helix.
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IDH1 inhibitor
Olutasidenib is a potent, selective inhibitor of mutant Isocitrate dehydrogenase (IDH)1 for the treatment of acute myeloid leukemia.
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MAO inhibitor
Iproniazid phosphate is an irreversible inhibitor of monoamine oxidase types A and B that is used as an antidepressive agent. It has also been used as an antitubercular agent, but its use is limited by its toxicity.
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MAO inhibitor
Iproniazid is a non-selective, irreversible monoamine oxidase (MAO) inhibitor (MAOI) that is used as an antidepressive agent.
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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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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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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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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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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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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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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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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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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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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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TrxR1/CRM1 抑制剂
Piperlongumine,存在于胡椒科植物荜茇中的一种天然生物碱,能够增加reactive oxygen species (ROS)水平,并选择性杀死癌细胞。它还是TrxR1的直接抑制剂,对胃癌具有抑制活性;一种新型的CRM1抑制剂;在人类乳腺癌细胞中可抑制PI3K/Akt/mTOR。
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AhR 拮抗剂
StemRegenin 1 (SR1)是一种细胞可渗透的嘌呤衍生物,作为芳香烃受体的拮抗剂,促进造血干细胞(HSC)的自我更新。
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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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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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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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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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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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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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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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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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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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Androgen Receptor 拮抗剂
Cyproterone acetate是17-羟孕酮的合成衍生物,可作为雄激素受体拮抗剂以及具有弱孕激素和糖皮质激素活性的弱孕激素受体激动剂。
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Naringenin是一种黄烷酮,是一种类黄酮,被认为具有抗氧化剂,自由基清除剂,消炎,碳水化合物代谢促进剂和免疫系统调节剂等对人体健康的生物活性。
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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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Anti-Diabetic Agent
Acarbose是一种肠道alpha-glucosidase抑制剂,用于治疗2型糖尿病以及某些国家的前驱糖尿病。
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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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