2755241-73-5

CASK-IN-1 is a highly potent and selective CASK inhibitor with a Kd value of 0.022 μM.

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.

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[1] Russ N, et al. Design and Development of a Chemical Probe for Pseudokinase Ca2+/calmodulin-Dependent Ser/Thr Kinase. J Med Chem. 2021 Oct 14;64(19):14358-14376. DOI:10.1021/acs.jmedchem.1c00845