SMI-4a


Catalog No. size PriceQuantity
M60416-2S 2 mg solid $79
M60416-10S 10mg solid $324

Description

Product Information
Molecular Weight: 273.23
Formula: C11H6F3NO2S
Purity: >98%
CAS#: 438190-29-5
Solubility: 10 mM in DMSO
Chemical Name: 5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month

 

Biological Activity:


(Z)-SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested. IC50 value: 21 nM (Pim1); 100 nM (Pim2) [1] Target: Pim-1 

How to use:

 in vitro: Incubation of pre-T-LBL cells with (Z)-SMI-4a induced G1 phase cell-cycle arrest secondary to a dose-dependent induction of p27(Kip1), apoptosis through the mitochondrial pathway, and inhibition of the mammalian target of rapamycin C1 (mTORC1) pathway based on decreases in phospho-p70 S6K and phospho-4E-BP1, 2 substrates of this enzyme. In addition, treatment of these cells with (Z)-SMI-4a was found to induce phosphorylation of extracellular signal-related kinase1/2 (ERK1/2), and the combination of (Z)-SMI-4a and a mitogen-activated protein kinase kinase 1/2 (MEK1/2) inhibitor was highly synergistic in killing pre-T-LBL cells [1]. Ectopic expression of phosphomimetic mutants of eIF4B conferred resistance to apoptosis by the Pim kinase inhibitor (Z)-SMI-4a in Abl-transformed cells [2].

in vivo: In immunodeficient mice carrying subcutaneous pre-T-LBL tumors, treatment twice daily with (Z)-SMI-4a caused a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries [1].

Reference:

[1]. Lin YW, et al. A small molecule inhibitor of Pim protein kinases blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. Blood. 2010 ;115(4):824-33.
[2]. Yang J, et al. eIF4B phosphorylation by pim kinases plays a critical role in cellular transformation by Abl oncogenes. Cancer Res. 2013 Aug 1;73(15):4898-908.

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