NR 162

Name: NR 162
Brand: Tocris Bioscience
SKU: 7572

Tocris Bioscience, part of Bio-Techne | Catalog # 7572

COA / SDS

Potent and selective calcium/calmodulin-dependent serine protein kinase (CASK) inhibitor

Key Product Details

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)
Molecular Weight:	610.35

View Full Technical Details for NR 162

Technical Data
Citations

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 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	4.10 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 Design and development of a chemical probe for pseudokinase Ca²⁺/calmodulin-dependent Ser/Thr kinase. J.Med.Chem. 2021 PMID: 34543009