LKB1 (AAK1 dual inhibitor)Pim-1 kinase inhibitor CAS# 1093222-27-5 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1093222-27-5 | SDF | Download SDF |
| PubChem ID | 44588117 | Appearance | Powder |
| Formula | C20H13N5O | M.Wt | 339.36 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | LKB1/AAK1 dual inhibitor | ||
| Solubility | DMSO : 50 mg/mL (147.34 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | N-[5-(4-cyanophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide | ||
| SMILES | C1=CC(=CN=C1)C(=O)NC2=CNC3=NC=C(C=C23)C4=CC=C(C=C4)C#N | ||
| Standard InChIKey | JTSLALYXYSRPGW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H13N5O/c21-9-13-3-5-14(6-4-13)16-8-17-18(12-24-19(17)23-11-16)25-20(26)15-2-1-7-22-10-15/h1-8,10-12H,(H,23,24)(H,25,26) | ||
| 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 | Pim1/AKK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.In Vitro:Pim1/AKK1-IN-1 is multi-kinase inhibitor, and has Kd of 380 nM against LKB1 and 53 nM against AAK1[1]. References: | |||||
| Kinase experiment [1]: | |
| Binding assays | Kinases were expressed as fusion proteins to T7 phage. In general, full-length constructs were used for small kinases and catalytic domains for large kinases. T7-kinase-tagged phage strains were mixed with known kinase inhibitors immobilized on streptavidin-coated magnetic beads and with LKB1 (AAK1 dual inhibitor) at a single concentration of 10 μM. LKB1 (AAK1 dual inhibitor) that bind to the kinase ATP site displace the immobilized ligand from the kinase/phage, which is detected using quantitative PCR. The results are reported as the percentage of kinase/phage remaining bound to the ligand/beads, relative to a control (DMSO). High affinity compounds have %control= 0, while weaker binders have higher %control values. Results are reported for screening against 203 human kinases. |
| References: [1]. Bamborough P, Drewry D, Harper G, et al. Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem, 2008, 51(24): 7898-7914. | |
LKB1 (AAK1 dual inhibitor) Dilution Calculator
LKB1 (AAK1 dual inhibitor) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.9467 mL | 14.7336 mL | 29.4672 mL | 58.9345 mL | 73.6681 mL |
| 5 mM | 0.5893 mL | 2.9467 mL | 5.8934 mL | 11.7869 mL | 14.7336 mL |
| 10 mM | 0.2947 mL | 1.4734 mL | 2.9467 mL | 5.8934 mL | 7.3668 mL |
| 50 mM | 0.0589 mL | 0.2947 mL | 0.5893 mL | 1.1787 mL | 1.4734 mL |
| 100 mM | 0.0295 mL | 0.1473 mL | 0.2947 mL | 0.5893 mL | 0.7367 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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LKB1 is a selective inhibitor of Pim-1 kinase with Kd value of 35 nM [1].
Pim-1 (proto-oncogene serine/threonine-protein kinase) is a proto-oncogene encodes by PIM1 gene and is reported to play an important role in multiple human cancers. Initially, pim-1 is reported to be expressed in spleen, thymus, bone marrow, prostate, oral epithelial cells, etc. Recently, the high expression of pim-1 has been identified in several isolated human cancer cells and been shown to involve in the cell cycle progression, apoptosis, transcriptional activation and many general signal transduction pathways. Therefore, investigation of the inhibition of pim-1 by low molecular weight compounds as a part of anticancer therapeutic strategies needs more attention and progress [2, 3].
References:
1. Bamborough, P., et al., Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. J Med Chem, 2008. 51(24): p. 7898-914.
2. Natarajan, K., et al., The Pim kinase inhibitor SGI-1776 decreases cell surface expression of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and drug transport by Pim-1-dependent and -independent mechanisms. Biochem Pharmacol, 2013. 85(4): p. 514-24.
3. Tsuganezawa, K., et al., A novel Pim-1 kinase inhibitor targeting residues that bind the substrate peptide. J Mol Biol, 2012. 417(3): p. 240-52.
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