H3B-120

Names

[ CAS No. ]:
2194903-42-7

[ Name ]:
H3B-120

Biological Activity

[Description]:

H3B-120 is a highly selective, competitive and allosteric carbamoyl phosphate synthetase 1 (CPS1) inhibitor with an IC50 of 1.5 μM and a Ki of 1.4 μM. H3B-120 has anti-cancer activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> Potassium Channel

[Target]

IC50: 1.5 μM (CPS1)[1] Ki: 1.4 μM (CPS1)[1]

[In Vitro]

H3B-120 has no inhibition of CPS2 activity of CAD (CPS2, aspartyl transcarbamylase, dihydroorotase)[1]. H3B-120 achieves inhibition by binding to an allosteric pocket situated between the integrating and ATP A domains[1]. H3B-120 (25, 50, 75, 100 μM) inhibits urea production in a dose-dependent manner, although the cellular potency decreases significantly compared with enzymatic assays[1]. The half-life of H3B-120 is only 40 min[1].

[References]

[1]. Yao S, et al. Small Molecule Inhibition of CPS1 Activity through an Allosteric Pocket. Cell Chem Biol. 2020 Mar 19;27(3):259-268.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₂₄N₄O₂S

[ Molecular Weight ]:
372.48

H3B-120

Names

Biological Activity

Chemical & Physical Properties

Related Compounds