TH1760

• CAT Number: I037184
• Molecular Formula: C20H18N4O5S
• Molecular Weight: 426.45
• Purity: 98%
• Synonyms: TH1760; TH 1760; TH-1760; MKB
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Storage: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
• IUPAC Name: 6-((4-(1H-indole-5-carbonyl)piperazin-1-yl)sulfonyl)benzo[d]oxazol-2(3H)-one
• InChI: InChI=1S/C20H18N4O5S/c25-19(14-1-3-16-13(11-14)5-6-21-16)23-7-9-24(10-8-23)30(27,28)15-2-4-17-18(12-15)29-20(26)22-17/h1-6,11-12,21H,7-10H2,(H,22,26)
• InChIKey: HNCVDRFFJZJQRW-UHFFFAOYSA-N
• SMILES: O=C1OC2=CC(S(=O)(N3CCN(C(C4=CC5=C(NC=C5)C=C4)=O)CC3)=O)=CC=C2N1

TH1760 (Cat No.: I037184) is a selective small-molecule inhibitor of Macrodomain 2 (MacroD2), an enzyme involved in ADP-ribosylation, a key post-translational modification linked to DNA repair and cellular stress responses. By inhibiting MacroD2, TH1760 disrupts the removal of ADP-ribose from target proteins, thereby modulating DNA damage response pathways. This makes it a valuable tool for studying PARP-related processes and exploring novel cancer treatment strategies. TH1760 is particularly useful in research focused on genomic stability, epigenetic regulation, and targeted cancer therapeutics.

Reference

1: Zhang SM, Desroses M, Hagenkort A, Valerie NCK, Rehling D, Carter M, Wallner O, Koolmeister T, Throup A, Jemth AS, Almlöf I, Loseva O, Lundbäck T, Axelsson H, Regmi S, Sarno A, Krämer A, Pudelko L, Bräutigam L, Rasti A, Göttmann M, Wiita E, Kutzner J, Schaller T, Kalderén C, Cázares-Körner A, Page BDG, Krimpenfort R, Eshtad S, Altun M, Rudd SG, Knapp S, Scobie M, Homan EJ, Berglund UW, Stenmark P, Helleday T. Development of a chemical probe against NUDT15. Nat Chem Biol. 2020 Oct;16(10):1120-1128. doi: 10.1038/s41589-020-0592-z. Epub 2020 Jul 20. PMID: 32690945.