5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮

• 常用名: 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
• 英文名: TCS-PIM-1-4a
• CAS号: 327033-36-3
• 分子量: 273.231
• 密度: 1.5±0.1 g/cm3
• 沸点: N/A
• 分子式: C₁₁H₆F₃NO₂S
• 熔点: N/A
• 闪点: N/A

用途

TCS-PIM-1-4a是Pim抑制剂,能通过AMPK的活化阻断 mTORC1活性,对各种骨髓和淋巴细胞株有杀伤活性,IC50从0.8到40 μM。

名称

• 中文名: 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮
• 英文名: SMI-4a

生物活性

• 描述: TCS-PIM-1-4a是Pim抑制剂,能通过AMPK的活化阻断 mTORC1活性,对各种骨髓和淋巴细胞株有杀伤活性,IC50从0.8到40 μM。
• 相关类别:
  信号通路 >> JAK/STAT信号通路 >> 皮姆
  研究领域 >> 癌症
• 参考文献:

  [1]. Lin YW, Beharry ZM, Hill EG, et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood. 2010 ;115(4):824-33.

  [2]. Beharry Z, Mahajan S, Zemskova M,et al. The Pim protein kinases regulate energy metabolism and cell growth. Proc Natl Acad Sci U S A. 2011;108(2):528-33.

  [3]. Benoit SR, Ji M, Fleming R,et al . Predictors of dropouts from a San Diego diabetes program: a case control study. Prev Chronic Dis. 2004:1(4):A10.

  [4]. Zuping Xia, Christian Knaak, Jian Ma et al. Synthesis and Evaluation of Novel Inhibitors of Pim-1 and Pim-2 Protein Kinases. J. Med. Chem., 2009, 52 (1), pp 74-86

物理化学性质

• 密度: 1.5±0.1 g/cm3
• 分子式: C₁₁H₆F₃NO₂S
• 分子量: 273.231
• 精确质量: 273.007141
• PSA: 71.47000
• LogP: 2.30
• InChIKey: NGJLOFCOEOHFKQ-VMPITWQZSA-N
• SMILES: O=C1NC(=O)C(=Cc2cccc(C(F)(F)F)c2)S1
• 折射率: 1.602
• 储存条件: 2-8℃

安全信息

• 海关编码: 2934999090

海关

• 海关编码: 2934999090
• 中文概述: 2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%
• 申报要素: 品名, 成分含量, 用途
• Summary: 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

靶点实验

查看更多实验

实验名称：Discovery of Small Molecules to Inhibit Human Cytomegalovirus Nuclear Egress 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：HCMV UL50 External Id：HMS1262

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VER... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4513082

实验名称：Chemical Probes of Kaposi's Sarcoma Herpes Virus Latent Infection 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：ORF 73 [Human herpesvirus 8 type M] External Id：HMS791

实验名称：Small-molecule inhibitors of ST2 (IL1RL1) 来源：20881 靶标：interleukin-1 receptor-like 1 isoform [homo sapiens] External Id：ST2_IL33_Inhibitors_Primary_Screening_77700

实验名称：High-throughput screen for inhibitors of the GIV GBA-motif interaction with Galpha-i ... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS1303

实验名称：Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Cac... 来源：ChEMBL 靶标：Severe acute respiratory syndrome coronavirus 2 External Id：CHEMBL4303805

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：Alphascreen assay for small molecules abrogating mHTT-CaM Interaction 来源：24983 靶标：Huntingtin External Id：KUHTS-Muma KU-CaM-Htt INH-01

实验名称：SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f... 来源：ChEMBL 靶标：Replicase polyprotein 1ab External Id：CHEMBL4495582

实验名称：A screen for compounds that inhibit viral RNA polymerase binding and polymerization a... 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School 靶标：Chain A, Poliovirus Polymerase With Gtp External Id：HMS750

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英文别名

• (5E)-5-[3-(Trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione
• TCS-PIM-1-4a
• (5Z)-5-[3-(Trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione