N-METHYL-N-[3-(3-METHYL[1,2,4]TRIAZOLO[4,3-B]PYRIDAZIN-6-YL)PHENYL]ACETAMIDE

• CAT Number: M010548
• CAS Number: 108825-65-6
• Molecular Formula: C15H15N5O
• Molecular Weight: 281.319
• Purity: ≥95%
• Synonyms: N-METHYL-N-[3-(3-METHYL[1,2,4]TRIAZOLO[4,3-B]PYRIDAZIN-6-YL)PHENYL]ACETAMIDE;Lin28 1632
• Storage: -20°C
• IUPAC Name: N-methyl-N-[3-(3-methyl-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)phenyl]acetamide
• InChI: InChI=1S/C15H15N5O/c1-10-16-17-15-8-7-14(18-20(10)15)12-5-4-6-13(9-12)19(3)11(2)21/h4-9H,1-3H3
• InChIKey: WPAQLESUVYGUJZ-UHFFFAOYSA-N
• SMILES: CC1=NN=C2N1N=C(C=C2)C3=CC(=CC=C3)N(C)C(=O)C

N-METHYL-N-[3-(3-METHYL[1,2,4]TRIAZOLO[4,3-B]PYRIDAZIN-6-YL)PHENYL]ACETAMIDE (CAS 108825-65-6), also known as Lin28 1632, is a small molecule inhibitor of the interaction between the RNA binding protein Lin28 and let-7 precursor RNA (IC50 = 8 μM in a competition ELISA).It increases levels of endogenous let-7 miRNAs and decreases Lin28 expression in a dose-dependent manner in murine embryonic stem cells (mESCs). Lin28 1632 inhibits clonogenic growth of 22Rv1, PC3, DU145, and Huh7 cancer cells and decreases tumor-sphere formation by 22Rv1 and Huh7 cells in vitro. It also binds bromodomain-containing protein 4 (BRD4) and CREB-binding protein (CBP/CREBBP) bromodomains (Kds = 7 and 25 μM, respectively).

Reference

1.Roos, Martina, et al. "A small-molecule inhibitor of Lin28." ACS chemical biology 11.10 (2016): 2773-2781.