Name | SMI-4a |
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Synonyms |
2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-, (5E)-
(5E)-5-[3-(Trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione TCS-PIM-1-4a (5Z)-5-[3-(Trifluoromethyl)benzylidene]-1,3-thiazolidine-2,4-dione 2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)phenyl]methylene]-, (5Z)- |
Description | TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activity via activation of AMPK; kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM).IC50 value:Target: Pim SMI-4a a novel benzylidene-thiazolidine-2, 4-dione small molecule inhibitor of the Pim kinases, kills a wide range of both myeloid and lymphoid cell lines with precursor T-cell lymphoblastic leukemia/lymphoma (pre-T-LBL/T-ALL) being highly sensitive. Incubation of pre-T-LBL cells with 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 SMI-4a was found to induce phosphorylation of extracellular signal-related kinase1/2 (ERK1/2), and the combination of SMI-4a and a mitogen-activated protein kinase kinase 1/2 (MEK1/2) inhibitor was highly synergistic in killing pre-T-LBL cells. SMI-4a blocked the rapamycin-sensitive mTORC1 activity by stimulating the phosphorylation and thus activating the mTORC1 negative regulator AMP-dependent protein kinase (AMPK). |
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Related Catalog | |
References |
Density | 1.5±0.1 g/cm3 |
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Molecular Formula | C11H6F3NO2S |
Molecular Weight | 273.231 |
Exact Mass | 273.007141 |
PSA | 71.47000 |
LogP | 2.30 |
Index of Refraction | 1.602 |
Storage condition | 2-8℃ |
HS Code | 2934999090 |
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HS Code | 2934999090 |
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Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |