Ceefourin 1

• 常用名: Ceefourin 1
• 英文名: Ceefourin 1
• CAS号: 315702-40-0
• 分子量: 294.419
• 密度: 1.6±0.1 g/cm3
• 沸点: 422.1±55.0 °C at 760 mmHg
• 分子式: C₁₁H₁₀N₄S₃
• 熔点: N/A
• 闪点: 209.1±31.5 °C

Ceefourin 1用途

Ceefourin 1 是一种有效且高度选择性的多药抗性蛋白 4 (MRP4) 抑制剂。Ceefourin 1 抑制多种 MRP4 底物的转运,但对其他 ABC 转运蛋白没有选择性。Ceefourin 1 是一种苯并噻唑,主要用作高危神经母细胞瘤的化学增敏剂。

Ceefourin 1名称

• 中文名: Ceefourin™1
• 英文名: 5-(Benzothiazol-2-ylsulfanylmethyl)-4-methyl-4H-[1,2,4]triazole-3-thiol

Ceefourin 1生物活性

• 描述: Ceefourin 1 是一种有效且高度选择性的多药抗性蛋白 4 (MRP4) 抑制剂。Ceefourin 1 抑制多种 MRP4 底物的转运,但对其他 ABC 转运蛋白没有选择性。Ceefourin 1 是一种苯并噻唑,主要用作高危神经母细胞瘤的化学增敏剂。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 其他 >> 其他
• 靶点实验:

  MRP4[1]

• 体外研究: ceefourin1对MRP4的选择性高于其他ABC转运蛋白,包括P-糖蛋白(P-gp)、ABCG2(乳腺癌耐药蛋白；BCRP)和MRP1(ABCC1)。Ceefourin 1具有有限的靶外效应和高稳定性[1]。Ceefourin 1(100nm-100μM)对两个正常人(HSF,MRC5),七个神经母细胞瘤(BE(2)-C,IMR-32,LAN-1,IMR-32,SK-N-SH,NBL-WN,SHEP)和四个其他人类癌细胞系(HEPG2,LNCap,SJ-G2,MCF7)具有低细胞毒性(IC50>50)[1]。在hek2.5μuricen细胞中。Ceefourin 1阻断D-荧光素外排,IC50为1.5μM[1]。
• 参考文献:

  [1]. Leanna Cheung, et al. High-throughput screening identifies Ceefourin 1 and Ceefourin 2 as highly selective inhibitors of multidrug resistance protein 4 (MRP4). Biochem Pharmacol. 2014 Sep 1;91(1):97-108.

  [2]. Tony Huynh, et al. CCI52 sensitizes tumors to 6-mercaptopurine and inhibits MYCN-amplified tumor growth. Biochem Pharmacol. 2020 Feb;172:113770.

Ceefourin 1物理化学性质

• 密度: 1.6±0.1 g/cm3
• 沸点: 422.1±55.0 °C at 760 mmHg
• 分子式: C₁₁H₁₀N₄S₃
• 分子量: 294.419
• 闪点: 209.1±31.5 °C
• 精确质量: 294.006744
• LogP: 1.85
• InChIKey: KVNBVHCJAUXKPJ-UHFFFAOYSA-N
• SMILES: Cn1c(CSc2nc3ccccc3s2)n[nH]c1=S
• 蒸汽压: 0.0±1.0 mmHg at 25°C
• 折射率: 1.827

Ceefourin 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

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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：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

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

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Ceefourin 1英文别名

• MFCD03984494
• 5-(Benzothiazol-2-ylsulfanylmethyl)-4-methyl-4H-[1,2,4]triazole-3-thiol
• 5-[(1,3-Benzothiazol-2-ylsulfanyl)methyl]-4-methyl-2,4-dihydro-3H-1,2,4-triazole-3-thione