HIF-1/2α-IN-2

• 常用名: HIF-1/2α-IN-2
• 英文名: HIF-1/2α-IN-2
• CAS号: 862974-22-9
• 分子量: 342.35
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₆H₁₁FN₄O₂S
• 熔点: N/A
• 闪点: N/A

HIF-1/2α-IN-2用途

HIF-1/2α-IN-2是HIF-1/2α的抑制剂。HIF-1/2α-IN-2通过靶向铁硫簇组件2(ISCA2),降低HIF-1/2β水平并诱导铁饥饿反应[1]。

HIF-1/2α-IN-2名称

• 英文名: HIF-1/2α-IN-2

HIF-1/2α-IN-2生物活性

• 描述: HIF-1/2α-IN-2是HIF-1/2α的抑制剂。HIF-1/2α-IN-2通过靶向铁硫簇组件2(ISCA2),降低HIF-1/2β水平并诱导铁饥饿反应[1]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> HIF/HIF脯氨酰-羟化酶
• 靶点实验:

  Iron Sulfur Cluster Assembly 2 (ISCA2), HIF-1/2α[1]

• 体外研究: HIF-1/2α-IN-2(化合物#1)(0-25μM；24小时)降低HIF-2α翻译而不是转录,VEGFA和POU5F1(HIF-2β靶基因)转录呈下降趋势,对EPAS1(HIF-1α)的影响不显著[1]。HIF-1/2α-IN-2(0-100μM,24小时)抑制由IC50值为3.9μM的HIF-2α铁反应元件(IRE)荧光素酶报告子驱动的荧光素素酶的产生,以阻断HIF-2β的IRE依赖性翻译[1]。HIF-1/2α-IN-2(0,10,50μM)保护ISCA2免受蛋白酶介导的(4μg/mL)降解,(1.5μM；24 h)靶向ISCA2诱导常氧786-0细胞中的铁和金属积累[1]。HIF-1/2α-IN-2(0-100μM；24小时)可抑制ISCA2,并通过铁沉降促进细胞死亡[1]。Western Blot分析[1]细胞系：常氧786-0细胞(20%O2)和缺氧ACHN细胞(或最后24小时1%O2诱导HIF表达)浓度：0、1、5、10、25μM培养时间：24小时结果：常氧细胞中HIF-2α、FTH1、ISCA2蛋白水平降低,IRP2蛋白水平升高,高浓度超过10μM。缺氧ACHN细胞在1μM时HIF-2α和FTH1水平升高。细胞活力测定[1]细胞株：Normoxia 786-0细胞浓度：0-100μM培养时间：24小时结果：通过诱导铁下垂抑制786-0的细胞活力,IC50值为22.0μM。
• 参考文献:

  [1]. Green YS, et al. ISCA2 inhibition decreases HIF and induces ferroptosis in clear cell renal carcinoma. Oncogene. 2022 Sep 12.

HIF-1/2α-IN-2物理化学性质

• 分子式: C₁₆H₁₁FN₄O₂S
• 分子量: 342.35
• InChIKey: TUNSTYGNRZSNSX-UHFFFAOYSA-N
• SMILES: COc1cccc2sc(Nc3nnc(-c4ccc(F)cc4)o3)nc12

HIF-1/2α-IN-2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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