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Description: Potent and selective calcium/calmodulin-dependent serine protein kinase (CASK) inhibitor
Chemical Name: 4-(Cyclopentylamino)-2-((2,5-dibromo-4-methylbenzyl)amino)-N-(3-(2-oxooxazolidin-3-yl)propyl)pyrimidine-5-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for NR 162
NR 162 is a potent and selective calcium/calmodulin-dependent serine protein kinase (CASK) inhibitor (IC50 = 80 nM); it exhibits no significant activity against related kinases MERTK, AXL and ABL1 and ~ 47-fold selectivity over TYRO3 (IC50 = 3.8 μM). NR 162 targets the unique pocket created by CASK GFG motif; it is a type-I inhibitor which stabilizes the active state of CASK without affecting the scaffolding function. NR 162 induces cell death in actively differentiating cells of the P19 neuronal differentiation model. NR 162 shows no toxicity in differentiated cells, or in cancer cells.
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the NR 162 probe summary on the SGC website.
Technical Data for NR 162
| M. Wt | 610.35 |
| Formula | C24H30Br2N6O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2755241-73-5 |
| PubChem ID | 155908701 |
| InChI Key | BPLPIBNWDLPUKP-UHFFFAOYSA-N |
| Smiles | O=C(C1=CN=C(N=C1NC2CCCC2)NCC3=CC(Br)=C(C=C3Br)C)NCCCN4CCOC4=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for NR 162
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 12.21 | 20 | |
| ethanol | 3.05 | 5 |
Preparing Stock Solutions for NR 162
The following data is based on the product molecular weight 610.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.19 mL | 40.96 mL | 81.92 mL |
| 1 mM | 1.64 mL | 8.19 mL | 16.38 mL |
| 2 mM | 0.82 mL | 4.1 mL | 8.19 mL |
| 10 mM | 0.16 mL | 0.82 mL | 1.64 mL |
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Product Datasheets for NR 162
References for NR 162
References are publications that support the biological activity of the product.
Russ et al (2021) Design and development of a chemical probe for pseudokinase Ca2+/calmodulin-dependent Ser/Thr kinase. J.Med.Chem. 64 14358 PMID: 34543009
If you know of a relevant reference for NR 162, please let us know.
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Keywords: NR 162, NR 162 supplier, NR162, type-I, inhibitor, inhibits, potent, selective, calcium/calmodulin-dependent, serine, protein, kinase, CASK, GFG, calmodulin, CaM, Kinase, 7572, Tocris Bioscience
Citations for NR 162
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