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。
SMI-16a (Synonyms: PIM1/2 Kinase Inhibitor VI) 纯度: 99.70%
SMI-16a是选择性的 Pim 激酶抑制剂,对Pim1,Pim2 和 PC3 细胞的IC50值分别为0.15,0.02 和48 μM。
SMI-16a Chemical Structure
CAS No. : 587852-28-6
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥880 | In-stock | |
5 mg | ¥800 | In-stock | |
10 mg | ¥1100 | In-stock | |
25 mg | ¥2000 | In-stock | |
50 mg | ¥3000 | In-stock | |
100 mg | ¥4500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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SMI-16a 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Epigenetics Compound Library
- Immunology/Inflammation Compound Library
- JAK/STAT Compound Library
- Kinase Inhibitor Library
- Anti-Cancer Compound Library
- Anti-Pancreatic Cancer Compound Library
- Targeted Diversity Library
生物活性 |
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively. |
IC50 & Target |
IC50: 0.15 μM (Pim1), 0.02 μM (Pim2), 48 μM (PC3 cells)[1] |
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体外研究 (In Vitro) |
SMI-16a has excellent potency for inhibition of both Pim-1 and Pim-2[1]. Treatment with Pim-2 short-interference RNA as well as the Pim inhibitor SMI-16a successfully restores osteoblastogenesis suppressed by all the above inhibitory factors and MM cells. The SMI-16a treatment potentiates BMP-2-mediated anabolic signaling while suppressing TGF-β signaling[2]. 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. |
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体内研究 (In Vivo) |
Mice tolerate intraperitoneal dose of SMI-16a is 50 mg/kg daily for 5 days, while 100 mg/kg is overtly toxic. Treatment of the animals with SMI-16a for 5 days per week reduces the growth of tumors by approximately 50% and does not cause a loss of body weight. Subchronic dosing with SMI-16a does not affect the levels of red, white blood cells, including lymphocytes, monocytes, and granulocytes, indicating that the compound does not have myelosuppressive effects. SMI-16a does not have toxicity toward the liver as the albumin, alkaline phosphatase, and alanine aminotransferase levels are unchanged [1]. SMI-16a effectively prevents bone destruction while suppressing MM tumor growth in MM animal models[2]. 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. |
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分子量 |
263.31 |
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Formula |
C13H13NO3S |
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CAS 号 |
587852-28-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (379.78 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
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。 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
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参考文献 |
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Kinase Assay [1] |
Recombinant human Pim-1 (Upstate) is incubated with S6 kinase/Rsk-2 peptide 2 (KKRNRTLTK) as the substrate in the presence 100 µM of compounds from the screening library, 1 µM ATP and 10 mM MgCl2 for 1 h. The Kinase-Glo luciferase kit is used to measure residual ATP levels after the kinase reaction[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. |
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Cell Assay [1] |
Human prostate cancer PC3 cells are seeded in 96-well tissue culture dishes at approximately 10% confluency and allowed to attach and recover for 24 h. Varying concentrations of the test compounds (SMI-16a) are then added to each well, and the plates are incubated for an additional 48 h. The number of surviving cells is determined by the MTS assay. The percentage of cells killed is calculated as the percentage decrease in MTS metabolism compared with control cultures[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 Administration [1] |
Mice: Female Balb/C mice are injected subcutaneously with JC cells suspended in PBS. After palpable tumor growth, animals are treated five days per week by intraperitoneal injection of vehicle alone or 50 mg/kg of SMI-16a.Whole body weights and tumor volume measurements are performed three times per week[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. |
参考文献 |
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