Catalog No.: PC-72550Not For Human Use, Lab Use Only.
Compound R80 (CTPS1-IN-R80) is a potent, selective inhibitor of CTPS1 (cytidine triphosphate synthase 1) with IC50 of 8.4 nM in RapdFire MS assays, >100-fold selectivity over CTPS2 (IC50=4.3 uM).
Compound R80 (CTPS1-IN-R80) is a potent, selective inhibitor of CTPS1 (cytidine triphosphate synthase 1) with IC50 of 8.4 nM in RapdFire MS assays, >100-fold selectivity over CTPS2 (IC50=4.3 uM).
R80 inhibited lymphocyte proliferation (Jurkat cells IC50=30 nM, human/mouse T-Cells IC50=258/175 nM) by preventing expansion of CTP pools via de novo synthesis by CTPS1, consistent with the potent inhibition of purified CTPS1.
CTPS1-I250T and CTPS2-T250I mutants was sufficient to invert the selectivity of R80 between the isoforms.
