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Chemical Structure : Compound R80
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).
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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.
| M.Wt | 486.565 | |
| Formula | C21H22N6O4S2 | |
| Appearance | Solid | |
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1. Eric M Lynch, et al. Proc Natl Acad Sci U S A. 2021 Oct 5;118(40):e2107968118.
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