CTP Synthetase-IN-1

CTP Synthetase-IN-1 is a potent, orally active cytidine 5'-triphosphate synthetase (CTPS) inhibitor with IC50s of 32 nM and 18 nM for human CTPS1 and human CTPS2, respectively. CTP Synthetase-IN-1 has anti-inflammatory effects[1].

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis

Research Areas >> Inflammation/Immunology

IC50: 32 nM (human CTPS1) and 18 nM (human CTPS2)[1]

CTP Synthetase-IN-1 (compound 27) inhibits rat CTPS1, rat CTPS2, mouse CTPS1, and mouse CTPS2 with IC50 values of 27 nM, 23 nM, 26 nM, and 33 nM, respectively[1].

CTP Synthetase-IN-1 (compound 27; 10-50 mg/kg; p.o; twice daily; for 18 days) shows significant pharmacological responses in collagen-induced arthritis (CIA) model[1]. Animal Model: Mouse collagen-induced arthritis (CIA) model[1] Dosage: 10 mg/kg and 50 mg/kg Administration: p.o; twice daily; for 18 days Result: Resulted in improvements in specific indicators of disease severity.

[1]. Andrew Novak, et al. Discovery and Optimization of Potent and Orally Available CTP Synthetase Inhibitors for Use in Treatment of Diseases Driven by Aberrant Immune Cell Proliferation. J Med Chem. 2022 Dec 22;65(24):16640-16650.