Compound R80 | CTPS1 inhibitor | Probechem Biochemicals

Chemical Structure : Compound R80

CAS No.: 2341943-12-0

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Compound R80 (CTPS1-IN-R80)

货号: 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).

规格	价格	库存
2 mg	￥3280	In stock
5 mg	￥5280	In stock
10 mg	￥8980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	486.565
分子式	C21H22N6O4S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(1-(2-(cyclopropanesulfonamido)thiazol-4-yl)cyclopropyl)-5-(6-ethoxypyrazin-2-yl)picolinamide

参考文献

1. Eric M Lynch, et al. Proc Natl Acad Sci U S A. 2021 Oct 5;118(40):e2107968118.

Compound R80 (CTPS1-IN-R80)

生物&药学活性

物理化学性质&存储条件

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Compound R80 (CTPS1-IN-R80)

生物&药学活性

物理化学性质&存储条件

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