SMI-4a
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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
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