Inz-1

• 常用名: Inz-1
• 英文名: Inz-1
• CAS号: 897776-15-7
• 分子量: 266.29
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₁₄N₂O₂
• 熔点: N/A
• 闪点: N/A

Inz-1用途

Inz-1 是一种有效的、选择性的酵母线粒体细胞色素 bc1 (mitochondrial cytochrome bc1) 抑制剂 (IC50=8.092 μM),优于对人的 (IC50=45.320 μM)。Inz-1 逆转白色念珠菌对氟康唑 (HY-B0101) 或其他三唑抗真菌试剂的耐药性。

Inz-1名称

• 英文名: Inz-1

Inz-1生物活性

• 描述: Inz-1 是一种有效的、选择性的酵母线粒体细胞色素 bc1 (mitochondrial cytochrome bc1) 抑制剂 (IC50=8.092 μM),优于对人的 (IC50=45.320 μM)。Inz-1 逆转白色念珠菌对氟康唑 (HY-B0101) 或其他三唑抗真菌试剂的耐药性。
• 相关类别:
  研究领域 >> 感染
  信号通路 >> 代谢酶/蛋白酶 >> 细胞色素P450
  信号通路 >> 抗感染 >> 真菌
• 靶点实验:

  IC50: 8.092 μM (yeast mitochondrial cytochrome bc1) IC50: 45.320 μM (human mitochondrial cytochrome bc1)[1]

• 体外研究: Inz-1(0-16μM；24小时)在以葡萄糖或甘油为唯一碳源的培养基中,抑制了酿酒酵母(菌株BY4741)和白色念珠菌(SC5314)的生长,而对葡萄糖的生长只有轻微的减缓作用[1]；24小时)在野生型和F90Y突变型线粒体中显示出以浓度依赖方式抑制酵母细胞色素B酶活性。它对酿酒酵母和白色念珠菌的细胞色素bc1均有抑制作用,其IC50值分别为2.5μM和8.0μM[1]。Inz-1(0-100μM；24小时)对酵母比人细胞色素bc1有选择性,它对人类细胞色素bc1活性的抑制作用很弱,IC50为45.3μM,比从HEK293人胚胎肾细胞中纯化的线粒体中白色念珠菌同源物的IC50高5.6倍[1]。Inz-1(0-100μM；24小时)在强迫呼吸条件下仅在32μM时抑制增殖,在该浓度下仅轻度抑制[1]。Inz-1对念珠菌(candida)具有较强的抗药性,其IC50值分别为8.092μM和45.320μM。对念珠菌和HepG2呼吸生长的抑制作用分别为1.655um和>32μM[1]。
• 参考文献:

  [1]. Benjamin M Vincent, et al. A Fungal-Selective Cytochrome Bc 1 Inhibitor Impairs Virulence and Prevents the Evolution of Drug Resistance.Cell Chem Biol. 2016 Aug 18;23(8):978-991.

Inz-1物理化学性质

• 分子式: C₁₆H₁₄N₂O₂
• 分子量: 266.29
• InChIKey: RBYOCUDWQCQSAM-UHFFFAOYSA-N
• SMILES: COC(=O)Cn1nc(-c2ccccc2)c2ccccc21
• 储存条件: -20°C，密封，干燥

Inz-1靶点实验

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实验名称：Primary cell-based high-throughput screening assay for identification of compounds th... 来源：Johns Hopkins Ion Channel Center 靶标：regulator of G-protein signaling 4 isoform 2 [Homo sapiens] External Id：JHICC_RGS_Act_HTS

实验名称：Luminescence-based cell-based primary high throughput screening assay to identify ago... 来源：The Scripps Research Institute Molecular Screening Center 靶标：mu-type opioid receptor isoform MOR-1 [Homo sapiens] External Id：OPRM1-OPRD1_AG_LUMI_1536_1X%ACT PRUN

实验名称：QFRET-based biochemical primary high throughput screening assay to identify exosite i... 来源：The Scripps Research Institute Molecular Screening Center 靶标：disintegrin and metalloproteinase domain-containing protein 17 preproprotein [Homo sapiens] External Id：ADAM17_INH_QFRET_1536_1X%INH PRUN

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

实验名称：uHTS identification of small molecule activators of the adaptive arm of the Unfolded ... 来源：Burnham Center for Chemical Genomics 靶标：N/A External Id：BCCG-A405-UPR-XBP1-PrimaryAgonist-Assay

实验名称：High throughput fluorescence intensity-based biochemical assay to screen for small mo... 来源：University of Pittsburgh Molecular Library Screening Center 靶标：furin (paired basic amino acid cleaving enzyme), isoform CRA_a [Homo sapiens] External Id：MH080376 Biochemical HTS for Inhibitors of the Proprotein Convertase Furin.

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

实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

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