A thymidylate kinase inhibitor
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YMU1

Item No. 21981

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[2-(4,6-dimethyl-3-oxoisothiazolo[5,4-b]pyridin-2(3H)-yl)acetyl]-1-piperazinecarboxylic acid, ethyl ester
CAS Number
902589-96-2
Molecular Formula
C17H22N4O4S
Formula Weight
378.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30 mg/mlDMF: 0.30 mg/mL
λmax
226, 254, 319 nm
SMILES
O=C(OCC)N1CCN(C(CN(SC2=C3C(C)=CC(C)=N2)C3=O)=O)CC1
InChi Code
InChI=1S/C17H22N4O4S/c1-4-25-17(24)20-7-5-19(6-8-20)13(22)10-21-16(23)14-11(2)9-12(3)18-15(14)26-21/h9H,4-8,10H2,1-3H3
InChi Key
XXUFNNVFZFVKGP-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $94

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    10 mg

    $148

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    Product Description

    YMU1 is an inhibitor of thymidylate kinase (TMPK; IC50 = 610 nM).1 It is selective for thymidylate kinase over thymidine kinase 1. YMU1 (2 and 10 µM) reduces deoxythymidine triphosphate (dTTP) levels by 30-40% in p58-/- HCT116 cells without affecting dATP, dGTP, or dCTP levels. It also sensitizes a variety of cancer cell lines to doxorubicin (Item No. 15007), including p53+/+ and p53-/- HCT116, HT-29, SaoS2, MDA-MB-231, and MDA-MB-468 cells. YMU1 reduces tumor growth in a p53-/- HCT116 mouse xenograft model when administered at a dose of 5 mg/kg three times per week for four weeks.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hu, C.M., Yeh, M.T., Tsao, N., et al. Tumor cells require thymidylate kinase to prevent dUTP incorporation during DNA repair. Cancer Cell. 22(1), 36-50 (2012).