TCS-PIM-1-4a

TCS-PIM-1-4a (SMI-4a) 是一种泛 Pim 激酶抑制剂，通过激活 AMPK 来阻断 mTORC1 的活性。 TCS-PIM-1-4a 可杀死多种髓系和淋巴系细胞系（IC50 值范围为 0.8 μM 至 40 μM）。

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库存: 现货

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5mg

￥500.00

400.00

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10mg

￥600.00

480.00

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50mg

￥2200.00

1760.00

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100mg

￥4012.00

3210.00

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货号: ajci8222
CAS: 327033-36-3
别名: 5-[[3-(三氟甲基)苯基]亚甲基]-2,4-噻唑烷二酮,SMI-4a
分子式: C11H6F3NO2S
分子量: 273.23
纯度: >98%
溶解度: ≥ 9.4mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM) [1][2].

TCS-PIM-1-4a (10 μM; 24-48 hours; 6812/2 cells and Jurkat cells) treatment increases the population of cells in the G1 phase from 44.3% to 68.4% and from 56.2% to 67.1% in 6812/2 and Jurkat, respectively. S-phase cells are decreased in 6812/2, whereas only small changes are seen in Jurkat cells consistent with the lesser G1 block[1].TCS-PIM-1-4a (5 μM; 6 hours; 6812/2 cells and Jurkat cells) induces cell death by the induction of apoptosis[1]. TCS-PIM-1-4a (5 μM; 4-8 hours; 6812/2 cells and Jurkat cells) prevents the increase in 4E-BP1 protein levels and inhibits mTOR-directed phosphorylation on Thr37/46[1].

TCS-PIM-1-4a (SMI-4a; 60 mg/kg; oral gavage; twice daily; for 21 days; nu/nu nude mice) treatment causes a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries[1].

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.