TCS PIM-1 1Pim-1 kinase inhibitor,ATP-competitve CAS# 491871-58-0 |
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Quality Control & MSDS
3D structure
Package In Stock
Number of papers citing our products
| Cas No. | 491871-58-0 | SDF | Download SDF |
| PubChem ID | 1235170 | Appearance | Powder |
| Formula | C18H11BrN2O2 | M.Wt | 367.2 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | SC 204330 | ||
| Solubility | DMSO : ≥ 52 mg/mL (141.61 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 6-(5-bromo-2-hydroxyphenyl)-2-oxo-4-phenyl-1H-pyridine-3-carbonitrile | ||
| SMILES | C1=CC=C(C=C1)C2=C(C(=O)NC(=C2)C3=C(C=CC(=C3)Br)O)C#N | ||
| Standard InChIKey | SVSYJTYGPLVUOZ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C18H11BrN2O2/c19-12-6-7-17(22)14(8-12)16-9-13(11-4-2-1-3-5-11)15(10-20)18(23)21-16/h1-9,22H,(H,21,23) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | ATP-competitive Pim-1 kinase inhibitor that displays selectivity over Pim-2 and MEK1/2 (IC50 values are 50, > 20000 and > 20000 nM for Pim-1, Pim-2 and MEK1/2 respectively). |
TCS PIM-1 1 Dilution Calculator
TCS PIM-1 1 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7233 mL | 13.6166 mL | 27.2331 mL | 54.4662 mL | 68.0828 mL |
| 5 mM | 0.5447 mL | 2.7233 mL | 5.4466 mL | 10.8932 mL | 13.6166 mL |
| 10 mM | 0.2723 mL | 1.3617 mL | 2.7233 mL | 5.4466 mL | 6.8083 mL |
| 50 mM | 0.0545 mL | 0.2723 mL | 0.5447 mL | 1.0893 mL | 1.3617 mL |
| 100 mM | 0.0272 mL | 0.1362 mL | 0.2723 mL | 0.5447 mL | 0.6808 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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TCS PIM-1 1 is a selective inhibitor of Pim-1 with IC50 value of 50 nM [1].
Pim-1 is a proto-oncogene serine/threonine-protein kinase and plays an important role in cell cycle progression, apoptosis, transcriptional activation and more general signal transduction pathways. It has been shown that Pim-1 over-expression is correlated with a variety of human cancers [2].
TCS PIM-1 1 is a potent Pim-1 inhibitor and has a better selectivity to Pim-1 than to Pim-2. It was revealed that TCS PIM-1 1 was the most potent inhibitor of Pim-1 by outlining the crystal structure and it was also shown that TCS PIM-1 1 had better inhibitory activity to Pim-1 compared with Pim-2 [1].
References:
[1]. Cheney, I.W., et al., Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase. Bioorg Med Chem Lett, 2007. 17(6): p. 1679-83.
[2]. Cen, B., et al., The Pim-1 protein kinase is an important regulator of MET receptor tyrosine kinase levels and signaling. Mol Cell Biol, 2014. 34(13): p. 2517-32.
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Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.[Pubmed:17251021]
Bioorg Med Chem Lett. 2007 Mar 15;17(6):1679-83.
A novel series of highly potent substituted pyridone Pim-1 kinase inhibitors is described. Structural requirements for in vitro activity are outlined as well as a complex crystal structure with the most potent Pim-1 inhibitor reported (IC(50)=50 nM). A hydrogen bond matrix involving the Pim-1 inhibitor, two water molecules, and the catalytic core, together with a potential weak hydrogen bond between an aromatic hydrogen on the R(1) phenyl ring and a main-chain carbonyl of Pim-1, accounts for the overall potency of this inhibitor.
