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TCS-PIM-1-4a

TCS-PIM-1-4a (SMI-4a) 是一种泛-Pim 激酶抑制剂，可通过激活 AMPK 来阻断 mTORC1的活性。它可杀死多种髓样和淋巴样细胞系，IC50值为 0.8 μM 至 40 μM。

CAS号

327033-36-3

分子式

C11H6F3NO2S

主要靶点

Apoptosis|Pim

仅限科研使用

Cat No : CM06000

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Synonyms

5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮|SMI-4a

验证数据展示

  • CAS No.: 327033-36-3

    TCS-PIM-1-4a
    CAS#: 327033-36-3

产品信息

TCS-PIM-1-4a, a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

CAS号 327033-36-3
分子式 C11H6F3NO2S
主要靶点 Apoptosis|Pim
主要通路 凋亡|JAK/STAT信号通路|表观遗传
分子量 273.23
纯度 99.89%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮|SMI-4a

靶点活性

Pim:0.8-40 μM

体外活性

One hour inhibitor treatment (0.5 μM) of HEK-293T cultures at the end of a 4 hour 32PO4 incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 μM) and more potent in PC3 human prostate cancer cell killing (IC50 = 17 vs. 48 μM with respective inhibitor).

溶解度

DMSO:55 mg/mL (201.3 mM)

参考文献

1.Lin YW, 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, 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.Xia Z, 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

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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