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Kinome profiling of BV2 cells treated with crizotinib or compound 32

ABSTRACT: Src homology 2 domain–containing inositol 5-phosphatase 1 (SHIP1), encoded by gene INPP5D, is a lipid phosphatase that negatively regulates immune receptor signaling in hematopoietic cells and microglia, which modulates downstream cellular proliferation, survival, and chemotaxis. Here, we report the optimization and characterization of a pyridyl–pyrazole-piperidine scaffold as a basis for SHIP1 ligands that demonstrate cellular target engagement, brain exposure, and evidence of a central pharmacodynamic response in vivo. Structure–activity relationship studies guided by biochemical and cellular assays using multiple human and murine SHIP1 protein constructs and cells identified compound 32 as a SHIP1-active ligand. To ensure that the cellular activity of compound 32 is not due to kinase inhibition in general within the context of BV2 mouse microglia cells, we executed a kinome profiling study of compound 32 compared to crizotinib as a positive control using BV2 cell lysates.

INSTRUMENT(S):

ORGANISM(S): Mus Musculus (mouse)

TISSUE(S): Cell Culture

SUBMITTER: Steven Angus

LAB HEAD: Timothy Richardson

PROVIDER: PXD071931 | Pride | 2026-04-03

REPOSITORIES: Pride

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			Action	DRS
	250327_Disha_BV2_1TAD1.raw	Raw
	250327_Disha_BV2_1TAD2.raw	Raw
	250327_Disha_BV2_1TAD3.raw	Raw
	250327_Disha_BV2_3TAD1.raw	Raw
	250327_Disha_BV2_3TAD2.raw	Raw

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Kinome profiling of BV2 cells treated with crizotinib or compound 32

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