NR 162

Pricing Availability   Qty
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)
Datasheet
Citations
Reviews

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.

Select a batch to recalculate based on the batch molecular weight:
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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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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