T3Inh-1

• 常用名: T3Inh-1
• 英文名: T3Inh-1
• CAS号: 50440-30-7
• 分子量: 476.48600
• 密度: 1.431g/cm3
• 沸点: 662.7ºC at 760mmHg
• 分子式: C₂₇H₂₀N₆O₃
• 熔点: N/A
• 闪点: 354.6ºC

T3Inh-1用途

T3Inh-1是ppGalNAc-T3(IC50=7µM)的有效和选择性抑制剂。T3Inh-1可降低组织细胞和小鼠体内的FGF23激素水平,且不会产生任何毒副作用。T3Inh-1还可以预防乳腺癌细胞。ppGalNAc-T3酶至少涉及两种医学上重要的途径：癌症转移和FGF23的稳定(调节血液中的磷酸盐水平)[1]。

T3Inh-1名称

• 英文名: 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide

T3Inh-1生物活性

• 描述: T3Inh-1是ppGalNAc-T3(IC50=7µM)的有效和选择性抑制剂。T3Inh-1可降低组织细胞和小鼠体内的FGF23激素水平,且不会产生任何毒副作用。T3Inh-1还可以预防乳腺癌细胞。ppGalNAc-T3酶至少涉及两种医学上重要的途径：癌症转移和FGF23的稳定(调节血液中的磷酸盐水平)[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 其他 >> 其他
• 体外研究: T3Inh-1(5µM；24-48小时；5µM；MDA-MB231细胞)非常有效,可抑制80%以上的迁移和98%的侵袭,但对细胞增殖没有明显影响[1]。T3Inh-1没有毒性,不影响HEK细胞增殖[1]。T3Inh-1(HEK细胞；6小时)增加FGF23的分裂[1]。
• 体内研究: T3Inh-1(25或50 mg/kg；i.p.)阻断ppGalNAc-T3介导的FGF23聚糖掩蔽,从而增加其切割[1]。动物模型：野生型C57BL/6六到八周大的小鼠[1]剂量：25或50 mg/kg给药：腹腔注射(在25和50 mg/ml的DMSO中溶解,然后用PEG400进一步稀释,产生5和10 mg/ml供注射用的储备)结果：在第二阶段导致切割/完整FGF23的比率显著增加试验浓度为25和50 mg/kg。
• 参考文献:

  [1]. Song L, et al. Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels. Elife. 2017;6:e24051. Published 2017 Mar 31.

T3Inh-1物理化学性质

• 密度: 1.431g/cm3
• 沸点: 662.7ºC at 760mmHg
• 分子式: C₂₇H₂₀N₆O₃
• 分子量: 476.48600
• 闪点: 354.6ºC
• 精确质量: 476.16000
• PSA: 124.76000
• LogP: 7.01970
• InChIKey: KUBNLSZSAIOAMS-UHFFFAOYSA-N
• SMILES: O=C(Nc1ccc(Nc2ccncc2)cc1)c1ccc(Nc2ccnc3ccc([N+](=O)[O-])cc23)cc1
• 折射率: 1.783

T3Inh-1靶点实验

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实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_AG_FLUO8_1536_1X%ACT PRUN

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实验名称：Fluorescence polarization to screen for inhibitor that competite the binding of FadD2... 来源：Broad Institute 靶标：FATTY-ACID-CoA LIGASE FADD28 (FATTY-ACID-CoA SYNTHETASE) External Id：2147-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfect... 来源：Broad Institute 靶标：N/A External Id：Bursicon-induced LGR2 mediated cAMP production in LGR-2/CRE6x-Luciferase co-transfected HEK293 cells Inhibition - 7011-01_Antagonist_SinglePoint_HTS_Activity

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T3Inh-1英文别名

• hms2860i06