iFSP1

• 常用名: iFSP1
• 英文名: iFSP1
• CAS号: 150651-39-1
• 分子量: 323.35100
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₃N₅
• 熔点: N/A
• 闪点: N/A

iFSP1用途

iFSP1 是 FSP1 (AIFM2) 的选择性有效抑制剂,EC50 值为 103 nM。iFSP1 可选择性地诱导过表达 FSP1 的 GPX4 敲除细胞发生铁死亡 (ferroptosis)。iFSP1 可增强多种人癌细胞系对铁死亡诱导剂的敏感度,如: (1S,3R)-RSL3 (HY-100218A)。

iFSP1名称

• 中文名: 1-氨基-3-(对甲苯基)苯并[4,5]咪唑并[1,2-a]吡啶-2,4-二甲腈
• 英文名: 1-amino-3-(p-tolyl)benzo[4,5]imidazo[1,2-a]pyridine-2,4-dicarbonitrile

iFSP1生物活性

• 描述: iFSP1 是 FSP1 (AIFM2) 的选择性有效抑制剂,EC50 值为 103 nM。iFSP1 可选择性地诱导过表达 FSP1 的 GPX4 敲除细胞发生铁死亡 (ferroptosis)。iFSP1 可增强多种人癌细胞系对铁死亡诱导剂的敏感度,如: (1S,3R)-RSL3 (HY-100218A)。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞凋亡 >> Ferroptosis
• 靶点实验:

  EC50: 103 nM (FSP1)[1]

• 体外研究: iFSP1(0.001-1μM；24小时)呈剂量依赖性抑制Gpx4基因敲除细胞的生长,但不抑制野生型细胞的生长。用铁下垂抑制剂Lip-1治疗可保护GPX4敲除细胞免受iFSP1诱导的铁下垂[1]。iFSP1(0.001-1μM；24小时)比FSP1基因缺失效率低,而FSP1基因敲除背景下iFSP1处理对RSL3诱导的铁下垂没有加性作用[1]。iFSP1(3μM；24小时)的治疗导致RSL3在一组基因工程(FSP1基因敲除)的人癌细胞中具有明显的毒性[1]。AIFM2：黄素蛋白凋亡诱导因子线粒体相关2是一个以前未被认识的抗铁依赖性基因。AIFM2,更名为铁下垂抑制蛋白1(FSP1)[1]细胞增殖试验[1]细胞系：野生型和Gpx4敲除的Pfa1或HT1080细胞过度表达FSP1–HA浓度：0.001-1μM培养时间：24小时结果：对仅依赖于FSP1功能的细胞(未检测到Gpx4表达)有毒。细胞活力测定[1]细胞系：NCl-H1437,NCl-H1437 FSP1 KO,U-373,U-373 FSP1 KO,MDA-MB-436,MDA-MB-436 FSP1 KO,SW620,SW620 FSP1 KO,MDA-MB-435S,MDA-MB-435S FSP1 KO,A549和A549 FSP1 KO浓度：3μM孵育时间：24小时结果：多种人癌细胞系对铁下垂诱导剂(1S,3R)-RSL3敏感。
• 参考文献:

  [1]. Doll S, et al. FSP1 is a glutathione-independent ferroptosis suppressor.Nature. 2019 Nov;575(7784):693-698.

iFSP1物理化学性质

• 分子式: C₂₀H₁₃N₅
• 分子量: 323.35100
• 精确质量: 323.11700
• PSA: 90.90000
• LogP: 4.36966
• InChIKey: FNESYDFRCQEEKA-UHFFFAOYSA-N
• SMILES: Cc1ccc(-c2c(C#N)c(N)n3c(nc4ccccc43)c2C#N)cc1
• 储存条件: 2-8℃，避光，干燥，密封

iFSP1安全信息

• 危害码 (欧洲): Xi

iFSP1靶点实验

查看更多实验

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：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

实验名称：Absorbance-based primary biochemical high throughput screening assay to identify acti... 来源：The Scripps Research Institute Molecular Screening Center 靶标：caspase-3 preproprotein [Homo sapiens] External Id：PROCASPASE3_ACT_EPIABS_1536_1X%ACT PRUN

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iFSP1英文别名

• MFCD01572665