2. Metabolic Enzyme/Protease
  3. PANK
  4. PZ-3022

PZ-3022 is an orally active allosteric agonist of pantothenate kinase (PanK) with an EC50 of 5.3 nM against PanK3. PZ-3022 antagonizes the inhibitory effect of C3-CoA. PZ-3022 increases CoA levels in cells and the liver, upregulates CoASH and C2-CoA, downregulates C3-CoA, and restores impaired TCA cycle and mitochondrial function. PZ-3022 can be used for the research of propionic acidemia and metabolic CoA deficiency.

For research use only. We do not sell to patients.

PZ-3022

PZ-3022 Chemical Structure

CAS No. : 2170608-85-0

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PZ-3022 Related Antibodies

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Description

PZ-3022 is an orally active allosteric agonist of pantothenate kinase (PanK) with an EC50 of 5.3 nM against PanK3. PZ-3022 antagonizes the inhibitory effect of C3-CoA. PZ-3022 increases CoA levels in cells and the liver, upregulates CoASH and C2-CoA, downregulates C3-CoA, and restores impaired TCA cycle and mitochondrial function. PZ-3022 can be used for the research of propionic acidemia and metabolic CoA deficiency[1][2].

In Vitro

PZ-3022 potently activates purified human PanK3 with an EC50 of 5.3 nM via allosteric binding to the PanK dimer[1].
PZ-3022 effectively elevates total intracellular CoA in cultured human C3A hepatoma cells and protects all PanK isoforms from C3-CoA-mediated inhibition[1].
PZ-3022 (compound 1) potently inhibits purified PANK3 enzyme with a Ki value of 5.3 nM; it also inhibits purified PANK1β enzyme with a Ki value of 789 nM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PZ-3022 Related Antibodies
In Vivo

PZ-3022 (10-30 mg/kg; p.o.; 3 doses at 24-hour intervals; short-term; 75 ppm in chow; daily administration; treatment from weaning to 70 days of age; long-term) modulates the hepatic coenzyme A pool, corrects abnormal acyl-carnitine ratios in liver and plasma, mitigates tricarboxylic acid cycle dysfunction, and alleviates cardiac phenotypic abnormalities in propionic acidemia mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Pcca-/-PCCA(A138T)tg/0 (male and female, weaned at 21 days, analyzed at 70 days of age, propionic acidemia model)[1]
Dosage: 10 mg/kg (short-term); 30 mg/kg (short-term); 75 ppm (long-term)
Administration: p.o.; 3 doses at 24-hour intervals (short-term); chow; daily; from weaning to 70 days of age (long-term)
Result: Raises hepatic CoASH, C2-CoA and total CoA, lowers hepatic C3-CoA, and optimizes hepatic C3:C2-CoA ratio in PA mice (short-term 10 or 30 mg/kg).
Decreases plasma C3:C2-carnitine ratio in male PA mice (short-term 30 mg/kg).
Returns hepatic CoASH and C2-CoA to baseline levels, reduces hepatic C3-CoA and hepatic C3:C2-CoA ratio in PA mice (long-term 75 ppm).
Modulates liver and plasma carnitine levels and cuts plasma C3:C2-carnitine ratio in PA mice of both sexes (long-term 75 ppm).
Lowers urinary TCA cycle metabolites with an 80% drop in malate and normalizes heart:body weight ratio in PA mice (long-term 75 ppm).
Molecular Weight

347.41

Formula

C20H21N5O
CAS No.
SMILES

N#CC1=NN=C(N2CCN(CC2)C(CC3=CC=C(C4CC4)C=C3)=O)C=C1
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References
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PZ-3022 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PZ-30222170608-85-0PZ3022PZ 3022PANKPantothenate Kinasehuman PANK3C57BL/6J micehuman PANK1βpropionyl-CoApantothenate kinaseCoASHCoApropionic acidemiaacetyl-CoAhuman C3A hepatoma cellsInhibitorinhibitorinhibit

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