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SMI 4A CAS NO.438190-29-5
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- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- SMI 4A
- (5Z)-5-[[3-(Trifluoromethyl)phenyl]methylene]-2,4-thiazolidinedione;TCS PIM-1 4a;SMI-4a;(Z)-5-(3-(trifluoroMethyl)benzylidene)thiazolidine-2,4-dione;2,4-Thiazolidinedione, 5-[[3-(trifluoromethyl)pheny
- 438190-29-5
Quick Details
- ProName: SMI 4A
- CasNo: 438190-29-5
- Molecular Formula: C11H6F3NO2S
- Appearance: white solid
- Application: CAS：438190-29-5； Small molecule inhib...
- DeliveryTime: 3 months
- PackAge: 100g,500g,1kg,25kg/drum
- Port: shang hai
- ProductionCapacity: 1000 Gram/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
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
in vitro: 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 [1]. Ectopic expression of phosphomimetic mutants of eIF4B conferred resistance to apoptosis by the Pim kinase inhibitor SMI-4a in Abl-transformed cells [2].
in vivo: In immunodeficient mice carrying subcutaneous pre-T-LBL tumors, treatment twice daily with SMI-4a caused a significant delay in the tumor growth without any change in the weight, blood counts, or chemistries [1].