TCS-PIM-1-4a(Synonyms: SMI-4a)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TCS-PIM-1-4a (Synonyms: SMI-4a) 纯度: 99.90%

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。TCS-PIM-1-4a 可杀死多种髓样和淋巴样细胞系 (IC50 值为 0.8 μM 至 40 μM)。

TCS-PIM-1-4a(Synonyms: SMI-4a)

TCS-PIM-1-4a Chemical Structure

CAS No. : 327033-36-3

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10 mM * 1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥810 In-stock
50 mg ￥2660 In-stock
100 mg ￥4700 In-stock
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TCS-PIM-1-4a 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library

生物活性

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].

IC50 & Target

Pim[1]
体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: 6812/2 cells and Jurkat cells
Concentration: 10 μM
Incubation Time: 24 hours, 48 hours
Result: Induced cell-cycle arrest.

Apoptosis Analysis[1]

Cell Line: 6812/2 cells and Jurkat cells
Concentration: 5 μM
Incubation Time: 6 hours
Result: Led to an increase in the number of the cells positive for annexin V and negative for PI from 8.25% in the control to 21.85%.

Western Blot Analysis[1]

Cell Line: 6812/2 cells and Jurkat cells
Concentration: 10 μM
Incubation Time: 4 hours, 8 hours
Result: Prevented the increase in 4E-BP1 protein levels and inhibited mTOR-directed phosphorylation on Thr37/46.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 18 Nu/nu nude mice with 6812/2 murine pre–T-LBL cells[1]
Dosage: 60 mg/kg
Administration: Oral gavage; twice daily; for 21 days
Result: Caused a significant delay in the tumor growth.

分子量

273.23

Formula

C11H6F3NO2S
CAS 号

327033-36-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (365.99 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6599 mL 18.2996 mL 36.5992 mL
5 mM 0.7320 mL 3.6599 mL 7.3198 mL
10 mM 0.3660 mL 1.8300 mL 3.6599 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.15 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.15 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (9.15 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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