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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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(Z)-SMI-4a (the Z-enantiomer of SMI-4a), a novel benzylidene-thiazolidine-2, 4-dione small molecule, is a potent and selective Pim1 inhibitor with potential antineoplastic activity. It inhibits Pim1 with an IC50 of 17 nM, it is modestly potent to Pim-2, and does not significantly inhibit any other serine/threonine- or tyrosine-kinases. SMI-4a blocks the growth of precursor T-cell lymphoblastic leukemia/lymphoma. SMI-4a was found to induce phosphorylation of extracellular signal-related kinase1/2 (ERK1/2). The serine/threonine Pim kinases are up-regulated in specific hematologic neoplasms, and play an important role in key signal transduction pathways, including those regulated by MYC, MYCN, FLT3-ITD, BCR-ABL, HOXA9, and EWS fusions. SMI-4a 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.
ln Vitro |
In intact cells, SMI-4a treatment (0.5 μM; 1 hour; HEK-293T cells) attenuates autophosphorylation of tagged Pim-1 [1].
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ln Vivo |
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Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK-293T cells Tested Concentrations: 0.5 µM Incubation Duration: 1 hour Experimental Results: Caused a dose-dependent reduction in Pim-1-induced 4E-BP1 phosphorylation, with an IC50 of approximately 125 nM. |
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Animal Protocol |
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References |
[1]. Xia Z, et al. Synthesis and evaluation of novel inhibitors of Pim-1 and Pim-2 protein kinases. J Med Chem. 2009 Jan 8;52(1):74-86.
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Molecular Formula |
C11H6F3NO2S
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Molecular Weight |
273.23
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CAS # |
438190-29-5
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Related CAS # |
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SMILES |
O=C(NC/1=O)SC1=C\C2=CC=CC(C(F)(F)F)=C2
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InChi Key |
NGJLOFCOEOHFKQ-VMPITWQZSA-N
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InChi Code |
InChI=1S/C11H6F3NO2S/c12-11(13,14)7-3-1-2-6(4-7)5-8-9(16)15-10(17)18-8/h1-5H,(H,15,16,17)/b8-5+
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Chemical Name |
5-(3-(trifluoromethyl)benzylidene)thiazolidine-2,4-dione
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Synonyms |
TCS PIM-1 4a; SMI-4a; SMI4a; SMI 4a
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6599 mL | 18.2996 mL | 36.5992 mL | |
5 mM | 0.7320 mL | 3.6599 mL | 7.3198 mL | |
10 mM | 0.3660 mL | 1.8300 mL | 3.6599 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
SMI-4a treatment inhibits the phosphorylation of TORC1 substrates.Blood.2010 Jan 28;115(4):824-33. td> |
SMI-4a treatment induces apoptosis in pre–T-LBL.Blood.2010 Jan 28;115(4):824-33. td> |
ERK1/2 phosphorylation is increased by SMI-4a treatment.Blood.2010 Jan 28;115(4):824-33. td> |
The sensitivity of leukemic cell lines to Pim kinase inhibitor SMI-4a.Blood.2010 Jan 28;115(4):824-33. td> |
SMI-4a treatment of pre–T-LBL down-regulates the level of MYC protein.Blood.2010 Jan 28;115(4):824-33. td> |
The in vivo sensitivity of 6812/2 to SMI-4a treatment.Blood.2010 Jan 28;115(4):824-33. td> |