526523
PIM1/2 Kinase Inhibitor V
(Z)-5-(3-Trifluoromethylbenzylidene)thiazolidine-2,4-dione, SMI-4a
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Merck KGaA
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15 February 2012
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A cell-permeable thiazolidinedione compound that acts as a potent, ATP-competitive inhibitor against Pim-1/2 kinases (IC50 = 24 nM and 100 nM against Pim-1 and Pim-2, respectively), while exhibiting little or no activity against a panel of 58 other kinases (≤20% inhibition at 5 µM). One hour inhibitor treatment (0.5 µM) of HEK-293T cultures at the end of a 4 hour 32PO4 incubation period results in nearly complete inhibition of the autophosphorylation of overexpressed Pim-1. Comparing to Inhibitor VI (Cat. No. 526524), Inhibitor V is less reactive towards DYRK1α (20% vs. 68% inhibition with respective inhibitor at 5 µM) and more potent in PC3 human prostate cancer cell killing (IC50 = 17 vs. 48 µM with respective inhibitor).
| Product information | |||
|---|---|---|---|
| Form | Light beige solid | ||
| Molar mass | 273.2 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥95% by HPLC | ||
| Solubility | DMSO | ||
| Chemical formula | C11H6F3NO2S | ||
| CAS number | 327033-36-3 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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