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)。
| 生物活性 | TCS-PIM-1-4a (SMI-4a) is a pan-Pimkinases inhibitor that blocksmTORC1activity via activation ofAMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50values ranging from 0.8 μM to 40 μM)[1][2]. |
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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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(365.99 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 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本网站选购。
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