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PZ-2891

Chemical Structure : PZ-2891

CAS No.: 2170608-82-7

PZ-2891 (PZ2891)

Catalog No.: PC-35831Not For Human Use, Lab Use Only.

PZ-2891 (PZ2891) a specific, allosteric, BBB-permeable, orally active Pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM, hPANK3) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical assays.

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Biological Activity

PZ-2891 (PZ2891) a specific, allosteric, BBB-permeable, orally active Pantothenate kinase (PANK) modulator, acting as both an orthosteric inhibitor (IC50=1.3 nM, hPANK3) and an allosteric activator of PANK3 activity in the presence of acetyl-CoA in biochemical assays.
PZ-2891 occupies the pantothenate pocket and engages the dimer interface to form a PANK•ATP•Mg2+•PZ-2891 complex.
PZ-2891 inhibits all 3 human and mouse pantothenate kinase isoforms (hPANK1α IC50=40.2 nM, hPANK2 IC50=0.7 nM).
PZ-2891 increases intracellular CoA in cultured cells and elevates CoA levels in mouse liver and brain, improves gain weight, locomotor activity and life span in mouse model of brain CoA deficiency.

Physicochemical Properties

M.Wt 349.438
Formula C20H23N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(4-(2-(4-isopropylphenyl)acetyl)piperazin-1-yl)pyridazine-3-carbonitrile

References

1. Sharma LK, et al. Nat Commun. 2018 Oct 23;9(1):4399.

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