HSP70-IN-1

• 常用名: HSP70-IN-1
• 英文名: HSP70-IN-1
• CAS号: 1268273-90-0
• 分子量: 464.583
• 密度: 1.3±0.1 g/cm3
• 沸点: N/A
• 分子式: C₂₄H₂₈N₆O₂S
• 熔点: N/A
• 闪点: N/A

HSP70-IN-1用途

HSP70-IN-1是一种热休克蛋白 (HSP) 抑制剂; 抑制Kasumi-1细胞的生长的IC50值为2.3 μM。

HSP70-IN-1名称

• 中文名: HSP70-IN-1
• 英文名: HSP70-IN-1

HSP70-IN-1生物活性

• 描述: HSP70-IN-1是一种热休克蛋白 (HSP) 抑制剂; 抑制Kasumi-1细胞的生长的IC50值为2.3 μM。
• 相关类别:
  研究领域 >> 癌症
• 靶点实验:

  HSP70

  Caspase-3/7:1.9 μM (IC50, MOLM13 cells)

• 体外研究: 热休克蛋白70(Hsp70)是分子伴侣,其在蛋白质稳态以及细胞信号传导和存活中起重要作用。 Hsp70经常在癌症中过表达,其中升高的表达还被认为是导致对化学疗法和其他治疗产生抗性的原因或导致对化疗和其他治疗的抗性。 HSP70-IN-1通过其剂量依赖性地改变巨型复合物组分并使Hsp70-Hsp90机器客户Raf-1不稳定的能力而干扰功能性Hsp70-HOP-Hsp90机制的形成。在细胞中,内源性和转染的Hsp70对热变性荧光素酶的重折叠被HSP70-IN-1抑制。 HSP70-IN-1还导致癌细胞中细胞凋亡的诱导。向癌细胞中添加HSP70-IN-1剂量依赖性地改变Hsp70-HOP复合物的形成,这是与其不稳定和半衰期减少相关的现象[1]。
• 参考文献:

  [1]. Taldone T, et al. Heat shock protein 70 inhibitors. 2. 2,5'-thiodipyrimidines, 5-(phenylthio)pyrimidines, 2-(pyridin-3-ylthio)pyrimidines, and 3-(phenylthio)pyridines as reversible binders to an allosteric site on heat shock protein 70. J Med Chem. 2014 Feb 27;57(4):1208-24.

HSP70-IN-1物理化学性质

• 密度: 1.3±0.1 g/cm3
• 分子式: C₂₄H₂₈N₆O₂S
• 分子量: 464.583
• 精确质量: 464.199432
• LogP: 3.27
• InChIKey: LBJCUDZMNPAWPX-UHFFFAOYSA-N
• SMILES: CN1CCN(c2ncc(Sc3cccc(NC(=O)CN)c3)c(OCc3ccccc3)n2)CC1
• 折射率: 1.686
• 储存条件: 2-8℃

HSP70-IN-1靶点实验

查看更多实验

实验名称：Inhibition of human HSP70 expressed in in HEK293 cells assessed as inhibition of refo... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128992

实验名称：Inhibition of HSP70 in HEK293 cells assessed as inhibition of refolding of heat denat... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128993

实验名称：Inhibition of HSP70 in human MOLM13 cells assessed as STAT5 degradation at 1 to 20 uM... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128994

实验名称：Inhibition of HSP70 in human MOLM13 cells assessed as mutant FLT3 degradation at 1 to... 来源：ChEMBL 靶标：Receptor-type tyrosine-protein kinase FLT3 External Id：CHEMBL3128995

实验名称：Inhibition of HSP70 in human MIAPaCa2 cells assessed as AKT degradation at 1 to 20 uM... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128996

实验名称：Inhibition of HSP70 in human MIAPaCa2 cells assessed as STAT-3 degradation at 1 to 20... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128997

实验名称：Inhibition of HSP70 in human MIAPaCa2 cells assessed as Raf-1 degradation at 1 to 20 ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128998

实验名称：Inhibition of HSP70 in human MDA-MB-468 cells assessed as Raf-1 degradation at 0.5 to... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3128999

实验名称：Inhibition of HSP70 in human MDA-MB-468 cells assessed as STAT-3 degradation at 0.5 t... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3129000

实验名称：Inhibition of HSP70 in human SKBR3 cells assessed as inhibition of HSP70-HOP-HSP90 co... 来源：ChEMBL 靶标：Heat shock protein HSP 90-alpha External Id：CHEMBL3129001

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HSP70-IN-1英文别名

• N-(3-{[4-(Benzyloxy)-2-(4-methyl-1-piperazinyl)-5-pyrimidinyl]sulfanyl}phenyl)glycinamide