HM03

• 常用名: HM03
• 英文名: HM03
• CAS号: 500565-15-1
• 分子量: 499.43200
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₆H₂₇ClN₄O₂
• 熔点: N/A
• 闪点: N/A

HM03用途

HM03 是一种有效的选择性的热休克 70 kDa 蛋白 5, HSPA5 (也称为 Bip,Grp78) 抑制剂,具有抗肿瘤活性。

HM03名称

• 英文名: 4-[(6-chloro-2-methoxyacridin-10-ium-9-yl)amino]-2-[(4-methylpiperazin-1-yl)methyl]phenol,chloride

HM03生物活性

• 描述: HM03 是一种有效的选择性的热休克 70 kDa 蛋白 5, HSPA5 (也称为 Bip,Grp78) 抑制剂,具有抗肿瘤活性。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 代谢酶/蛋白酶 >> HSP
  信号通路 >> 细胞周期/DNA损伤 >> HSP
• 靶点实验:

  HSPA5

• 体外研究: HM03(0.1-50μM；72小时)在浓度为25μM的HCT116细胞中表现出超过50%的抑制作用[1]。与其他HSP70蛋白相比,HM03与HSPA5和HSPA9形成更多的结合相互作用[1]。从癌细胞活性和肿瘤抑制试验来看,HM03具有很好的抑制活性[1]。细胞活力测定[1]细胞系：HCT116细胞浓度：0.1、1、10、25、50μM孵育时间：72小时结果：具有显著的抑制作用(25µM条件下存活率为18%)。
• 参考文献:

  [1]. Huang M, et al. Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors. Bioorg Med Chem Lett. 2013;23(10):3044‐3050.

HM03物理化学性质

• 分子式: C₂₆H₂₇ClN₄O₂
• 分子量: 499.43200
• 精确质量: 498.15900
• PSA: 64.09000
• LogP: 5.34630
• InChIKey: SUSDGTMJKOGWSZ-UHFFFAOYSA-N
• SMILES: COc1ccc2nc3cc(Cl)ccc3c(Nc3ccc(O)c(CN4CCN(C)CC4)c3)c2c1

HM03靶点实验

查看更多实验

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：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：Primary Screen Inhibitors of CD40 Signaling in BL2 Cells Measured in Cell-Based Syste... 来源：Broad Institute 靶标：N/A External Id：7124-01_Inhibitor_SinglePoint_HTS_Activity

实验名称：Antimicrobial activity against Escherichia coli 1411 after 18 hrs by broth microdilut... 来源：ChEMBL 靶标：Escherichia coli External Id：CHEMBL1821397

实验名称：Inhibition of Escherichia coli DdlB assessed as residual activity of the enzyme asses... 来源：ChEMBL 靶标：N/A External Id：CHEMBL1821396

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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