LSN 3213128（Cat No.:I018509）is a selective inhibitor targeting the histone methyltransferase EZH2, which plays a crucial role in regulating gene expression and cell proliferation in various cancers. By inhibiting EZH2, LSN 3213128 disrupts the methylation of histones, leading to reactivation of tumor suppressor genes and reduced cancer cell growth. Preclinical studies have shown its efficacy in models of hematological malignancies and solid tumors, particularly those with mutations in the EZH2 gene. Ongoing research aims to further investigate its therapeutic potential and optimize its application in cancer treatment regimens.
| Catalog Number | I018509 |
| CAS Number | 1941211-99-9 |
| Molecular Formula | C₁₇H₁₆FN₃O₄S₂ |
| Purity | ≥95% |
| IUPAC Name | N-(6-fluoro-1-oxo-2H-isoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide |
| InChI | InChI=1S/C17H16FN3O4S2/c18-13-7-10-3-5-19-17(23)12(10)8-14(13)20-27(24,25)16-2-1-15(26-16)21-6-4-11(22)9-21/h1-3,5,7-8,11,20,22H,4,6,9H2,(H,19,23)/t11-/m1/s1 |
| InChIKey | DSUZLJDXUJUTGI-LLVKDONJSA-N |
| SMILES | C1CN(C[C@@H]1O)C2=CC=C(S2)S(=O)(=O)NC3=C(C=C4C=CNC(=O)C4=C3)F |
| Reference | [1]. Fales KR, et al. Discovery of N-(6-Fluoro-1-oxo-1,2-dihydroisoquinolin-7-yl)-5-[(3R)-3-hydroxypyrrolidin-1-yl]thiophene-2-sulfonamide (LSN 3213128), a Potent and Selective Nonclassical Antifolate Aminoimidazole-4-carboxamide Ribonucleotide Formyltransferase (AICARFT) Inhibitor Effective at Tumor Suppression in a Cancer Xenograft Model. J Med Chem. 2017 Dec 14;60(23):9599-9616. |
