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SMI-4a
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SMI-4a图片
CAS NO:438190-29-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
SMI-4a 是一种强效、选择性、细胞渗透性和 ATP 竞争性 Pim-1 抑制剂，IC50 为 24 μM 和 Ki 为 0.6 μM。 SMI-4a 还抑制 Pim-2（IC50 为 100 μ；M），并且不显着抑制其他丝氨酸/苏氨酸或酪氨酸激酶。 SMI-4a 具有抗癌活性。
Cas No.438190-29-5
化学名5-[[3-(trifluoromethyl)phenyl]methylidene]-1,3-thiazolidine-2,4-dione
Canonical SMILESC1=CC(=CC(=C1)C(F)(F)F)C=C2C(=O)NC(=O)S2
分子式C11H6F3NO2S
分子量273.23
溶解度≥ 13.65 mg/mL in DMSO, ≥ 47.1 mg/mL in EtOH
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SMI-4a is a selective inhibitor of Pim1 with IC50 value of 17 nM [1] [2].

Pim-1 is an enzyme that is encoded by human PIM1 gene and it has been revealed that Pim-1 directly involved in the regulation of cell cycle progression and apoptosis and many studies have shown that Pim were over-expressed and promote cell growth and survival in a veraity of solid cancers and hematologic malignancies [3, 4].

SMI-4a is a selective Pim inhibitor and more active than the reported SMI-16a. When tested with human erythroleukemia cell line K562 cells, SIM-4a treatment modulated cell growth and activated AMPK which inhibited mTORC1 activity by inhibiting Pim activity [5]. In 25 leukemic cell lines, administration of SMI-4a induced cell-cycle arrest, elevated cell apoptosis, and pre–T-LBL/T-ALL being the highly sensitive cell line through mitochondrial pathway and inhibition of the mTORC1 pathway [2].

In Nu/nu nude mice model with 2 × 106 6812/2 cells subcutaneous xenograft, oral administration of SMI-4a from the third day for 5 of 7 days per week until day 21 on twice daily schedule significantly reduced tumor sizse [2].

References:
[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.