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DHODH-IN-1

Names

[ CAS No. ]:
1800296-63-2

[ Name ]:
DHODH-IN-1

Biological Activity

[Description]:

DHODH-IN-1 (compound 18d) is a potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 25 nM. DHODH-IN-1 is an inhibitor of pyrimidine biosynthesis pathway[1].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis
Signaling Pathways >> Metabolic Enzyme/Protease >> Lactate Dehydrogenase

[Target]

IC50: 25 nM (DHODH)[1]


[In Vitro]

DHODH-IN-1 (compound 18d) strongly inhibits Jurkat cells proliferation (IC50=0.02 μM)[1]. DHODH-IN-1 (4, 20, 100 nM) blocks the measles virus replication in cells[1]. DHODH-IN-1 (0.008, 0.04, 0.2, 1, 5 μM) increases the expression of an ISRE-luciferase reporter gene when transfecting cells with ssRNA molecules[1]. Cell Proliferation Assay[1] Cell Line: Jurkat cells Concentration: 0.00001, 0.0001, 0.001, 0.01, 0.1, 1, 10 μM Incubation Time: 72 hours Result: Strongly inhibited Jurkat cells proliferation (IC50=0.02 μM).

[In Vivo]

DHODH-IN-1 (compound 18d) has a t1/2 of 27–41 min[1].

[References]

[1]. Lucas-Hourani M, et al.Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH).J Med Chem. 2015 Jul 23;58(14):5579-98.

Chemical & Physical Properties

[ Molecular Formula ]:
C21H20F3N3O2

[ Molecular Weight ]:
403.40


Related Compounds