For research use only. Not for therapeutic Use.
LY 345899（Cat No.:I019965）is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), an enzyme critical for de novo purine biosynthesis. By targeting GARFT, LY 345899 disrupts the production of purine nucleotides, which are essential for DNA and RNA synthesis in rapidly dividing cells, making it a valuable compound in cancer research. Its ability to inhibit cell proliferation has shown promise in preclinical studies for the treatment of certain cancers, particularly in combination with other chemotherapeutic agents. LY 345899 offers a potential therapeutic strategy in oncology targeting nucleotide synthesis pathways.
| Catalog Number | I019965 |
| CAS Number | 10538-99-5 |
| Molecular Formula | C₂₀H₂₁N₇O₇ |
| Purity | ≥95% |
| Target | Methylenetetrahydrofolate Dehydrogenase (MTHFD) |
| Storage | Store at -20°C |
| IUPAC Name | (2S)-2-[[4-(3-amino-1,9-dioxo-5,6,6a,7-tetrahydro-2H-imidazo[1,5-f]pteridin-8-yl)benzoyl]amino]pentanedioic acid |
| InChI | InChI=1S/C20H21N7O7/c21-19-24-15-14(17(31)25-19)27-11(7-22-15)8-26(20(27)34)10-3-1-9(2-4-10)16(30)23-12(18(32)33)5-6-13(28)29/h1-4,11-12H,5-8H2,(H,23,30)(H,28,29)(H,32,33)(H4,21,22,24,25,31)/t11?,12-/m0/s1 |
| InChIKey | JSNFRYBHBVDHSG-KIYNQFGBSA-N |
| SMILES | C1C2CN(C(=O)N2C3=C(N1)N=C(NC3=O)N)C4=CC=C(C=C4)C(=O)N[C@@H](CCC(=O)O)C(=O)O |
| Reference | [1]. Schmidt A, et al. Structures of three inhibitor complexes provide insight into the reaction mechanism of the human methylenetetrahydrofolate dehydrogenase/cyclohydrolase. Biochemistry. 2000 May 30;39(21):6325-35.<br>[2]. Tedeschi PM, et al. Mitochondrial Methylenetetrahydrofolate Dehydrogenase (MTHFD2) Overexpression Is Associated with Tumor Cell Proliferation and Is a Novel Target for Drug Development. Mol Cancer Res. 2015 Oct;13(10):1361-6.<br>[3]. Gustafsson R, et al. Crystal Structure of the Emerging Cancer Target MTHFD2 in Complex with a Substrate-Based Inhibitor. Cancer Res. 2017 Feb 15;77(4):937-948.<br>[4]. Huai-Qiang Ju, et al.Modulation of Redox Homeostasis by Inhibition of MTHFD2 in Colorectal Cancer: Mechanisms and Therapeutic Implications. J Natl Cancer Inst. 2019 Jun 1;111(6):584-596. |
