Date published: 2026-4-1

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CPS1 Inhibitors

The CPS1 Inhibitors represent a diverse array of chemicals with distinct mechanisms of action, all geared towards modulating cellular processes that lead to the inhibition of carbamoyl phosphate synthetase 1 (CPS1). These inhibitors can be broadly categorized into direct and indirect inhibitors, each offering unique insights into potential strategies for regulating CPS1 activity. Direct inhibitors include well-established compounds such as DON (6-Diazo-5-oxo-L-norleucine), N-(phosphonoacetyl)-L-aspartate, Acivicin, and PALA (N-(Phosphonacetyl)-L-aspartate). DON, a glutamine analog, competes with glutamine, inhibiting CPS1 and disrupting the urea cycle. N-(phosphonoacetyl)-L-aspartate mimics the transition state of the substrate, competitively inhibiting CPS1's catalytic activity. Acivicin covalently modifies the active site of CPS1, leading to irreversible inactivation. PALA, a structural analog of aspartate, competitively inhibits CPS1, interfering with the urea cycle progression.

Indirect inhibitors showcase diverse mechanisms, including disruption of cellular pyridoxal phosphate levels (3-mercaptopyruvate and oxalate), interference with mitochondrial function (Methylene blue, 2,3-Butanedione monoxime, and Dichloroacetate), alteration of nucleotide pools (Hydroxyurea), inhibition of ribonucleotide reductase (Hydroxyurea), and modulation of ammonia metabolism (Acetohydroxamic acid and Oxalate). These chemicals collectively contribute to the dysregulation of CPS1 activity by influencing the biochemical and cellular pathways associated with urea cycle function. In summary, the CPS1 Inhibitors offer a comprehensive view of the strategies employed to modulate CPS1 activity directly or indirectly.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

6-Diazo-5-oxo-L-norleucine

157-03-9sc-227078
sc-227078A
sc-227078B
sc-227078C
5 mg
25 mg
100 mg
250 mg
$88.00
$291.00
$926.00
$2195.00
(0)

DON is a glutamine analog and a well-known inhibitor of carbamoyl phosphate synthetase 1 (CPS1). As a structural mimic of glutamine, DON competitively inhibits CPS1, preventing the conversion of ammonia and bicarbonate into carbamoyl phosphate. This inhibition disrupts the urea cycle, leading to the buildup of toxic ammonia and highlighting DON's potential as a direct inhibitor of CPS1.

Acivicin

42228-92-2sc-200498B
sc-200498C
sc-200498
sc-200498D
1 mg
5 mg
10 mg
25 mg
$104.00
$416.00
$655.00
$1301.00
10
(2)

Acivicin is a glutamine analog that covalently modifies the active site of CPS1, leading to the enzyme's irreversible inactivation. Through its mechanism of action, Acivicin provides a direct inhibitory effect on CPS1, disrupting the urea cycle and impairing the conversion of ammonia and bicarbonate into carbamoyl phosphate.

Hydroxyurea

127-07-1sc-29061
sc-29061A
5 g
25 g
$78.00
$260.00
18
(1)

Hydroxyurea, a ribonucleotide reductase inhibitor, indirectly influences CPS1 by perturbing deoxyribonucleotide synthesis. The inhibition of ribonucleotide reductase by hydroxyurea leads to altered nucleotide pools and increased orotate levels. This metabolic disturbance indirectly affects CPS1, disrupting the urea cycle and contributing to the dysregulation of ammonia metabolism.

Methylene blue

61-73-4sc-215381B
sc-215381
sc-215381A
25 g
100 g
500 g
$43.00
$104.00
$328.00
3
(1)

Methylene blue, a redox-active dye, indirectly inhibits CPS1 by disrupting the electron transport chain. By acting as an electron acceptor, methylene blue interferes with mitochondrial function, leading to decreased ATP production and the subsequent inhibition of CPS1. This disruption of cellular energetics indirectly impairs the urea cycle, preventing the conversion of ammonia and bicarbonate into carbamoyl phosphate.

2,3-Butanedione 2-Monoxime

57-71-6sc-203774
sc-203774A
sc-203774B
sc-203774C
25 g
100 g
250 g
500 g
$42.00
$78.00
$161.00
$286.00
(1)

2,3-Butanedione monoxime is an indirect inhibitor of CPS1 that disrupts the urea cycle by interfering with mitochondrial function. It has been shown to inhibit CPS1 activity by affecting the mitochondrial inner membrane potential, leading to impaired urea synthesis. This indirect inhibition prevents the conversion of ammonia and bicarbonate into carbamoyl phosphate, contributing to the dysregulation of nitrogen metabolism.

Dichloroacetic acid

79-43-6sc-214877
sc-214877A
25 g
100 g
$61.00
$128.00
5
(0)

Dichloroacetate is a pyruvate dehydrogenase kinase inhibitor that indirectly influences CPS1 by altering cellular energy metabolism. By inhibiting pyruvate dehydrogenase kinase, dichloroacetate promotes pyruvate dehydrogenase activity, leading to increased acetyl-CoA production. This metabolic shift indirectly affects CPS1, disrupting the urea cycle and impairing the conversion of ammonia and bicarbonate into carbamoyl phosphate.