SMI-4a
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
SMI-4a是PIM1的选择性抑制剂,IC 50值为17 nM[1,2]。
PIM-1是由人PIM1基因编码的酶。研究表明,PIM-1直接参与细胞周期和凋亡进程,在实体癌和恶性血液病中,PIM激酶的过表达可促进细胞生长和存活[3,4]。
SMI-4a是PIM激酶的选择性抑制剂,相较于SMI-16a具有更强的活性。在人红白血病细胞系K562中,SIM-4a通过抑制PIM的活性,进而抑制mTORC1的活性,参与调节细胞生长和激活AMPK [5]。在25白血病细胞系中,SMI-4a诱导细胞周期停滞,促进细胞凋亡。在淋巴母细胞淋巴瘤T-LBL/ T-ALL中,SMI-4a通过线粒体途径和抑制mTORC1发挥较高的选择性 [2]。
在使用2 × 106 6812/2细胞进行皮下异种移植的Nu/nu裸鼠模型中,从第三天口服SMI-4a,每天两次,每周5 -7天,直至第21天肿瘤体积显著下降[2]。
参考文献:
[1].Beharry, Z., et al., Novel benzylidene-thiazolidine-2,4-diones inhibit Pim protein kinase activity and induce cell cycle arrest in leukemia and prostate cancer cells. Mol Cancer Ther, 2009. 8(6): p. 1473-83.
[2].Lin, Y.W., et al., A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood, 2010. 115(4): p. 824-33.
[3].Liu, Z., et al., Computational prediction and experimental validation of a novel synthesized pan-PIM inhibitor PI003 and its apoptosis-inducing mechanisms in cervical cancer. Oncotarget, 2015.
[4].Warfel, N.A. and A.S. Kraft, PIM kinase (and Akt) biology and signaling in tumors. Pharmacol Ther, 2015.
[5].Beharry, Z., et al., The Pim protein kinases regulate energy metabolism and cell growth. Proc Natl Acad Sci U S A, 2011. 108(2): p. 528-33.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 273.23 |
Cas No. | 438190-29-5 |
Formula | C11H6F3NO2S |
Solubility | insoluble in H2O; ≥13.65 mg/mL in DMSO; ≥47.1 mg/mL in EtOH |
Chemical Name | 5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione |
SDF | Download SDF |
Canonical SMILES | C1=CC(=CC(=C1)C(F)(F)F)C=C2C(=O)NC(=O)S2 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
描述 | SMI-4a是Pim激酶的抑制剂。 | |||||
靶点 | Pim kinase | |||||
IC50 |
质量控制和MSDS
- 批次:
化学结构
![SMI-4a](http://www.apexbt.com//media/diy/images/struct/A4193.png)