PZ-2891

PZ-2891 is a modulator of pantothenate kinase (PanK). It selectively inhibits PanK1beta, 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.Formal Name: 6-[4-[2-[4-(1-methylethyl)phenyl]acetyl]-1-piperazinyl]-3-pyridazinecarbonitrile. CAS Number: 2170608-82-7. Synonyms: Pantazine 2891. Molecular Formula: C20H23N5O. Formula Weight: 349.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 10 mg/ml, DMSO: 2 mg/ml. lambdamax: 214, 285 nm. SMILES: N#CC1=CC=C(N2CCN(CC2)C(CC3=CC=C(C(C)C)C=C3)=O)N=N1. InChi Code: InChI=1S/C20H23N5O/c1-15(2)17-5-3-16(4-6-17)13-20(26)25-11-9-24(10-12-25)19-8-7-18(14-21)22-23-19/h3-8,15H,9-13H2,1-2H3. InChi Key: LGWDVWIZDPGCFG-UHFFFAOYSA-N.