NR 162

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

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