Formulation: A solid
Formal Name: 6-[4-[2-[4-(1-methylethyl)phenyl]acetyl]-1-piperazinyl]-3-pyridazinecarbonitrile
Purity: ≥98%
Formula Markup: C20H23N5O
Formula Weight: 349,4
Shelf life (days): 1460
CAS Number: 2170608-82-7
Notes: PZ-2891 is a modulator of pantothenate kinase (PanK).{51463} It selectively inhibits PanK1β, PanK2, and PanK3 (IC50s = 40.2, 0.7, and 1.3 nM, respectively) in the absence of acetyl-CoA over 468 other kinases and a panel of 72 receptors and ion channels at 10 µM. PZ-2891 (2.5 µM) reverses acetyl-CoA-induced inhibition of PanK3 in a cell-free assay, indicating activation of PanK3 activity. It increases intracellular CoA levels in wild-type PanK3-expressing HEK293T cells, but not in HEK293T cells expressing the catalytically inactive mutant PanK3E138A. PZ-2891 increases survival in a mouse model of neuronal CoA deficiency induced by brain knockout of Pank1 and Pank2. It prevents infection of mosquitoes (A. stephensi) by P. falciparum.{51464}
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