UZH1

• CAT Number: I044555
• CAS Number: 2925713-02-4
• Molecular Formula: C32H42N6O3
• Molecular Weight: 558.71
• Purity: ≥95%
• Synonyms: N-[[1-[6-(benzylamino)pyrimidin-4-yl]-3-hydroxypiperidin-3-yl]methyl]-4-[(4,4-dimethylpiperidin-1-yl)methyl]-2-hydroxybenzamide
• InChI: InChI=1S/C32H42N6O3/c1-31(2)12-15-37(16-13-31)20-25-9-10-26(27(39)17-25)30(40)34-21-32(41)11-6-14-38(22-32)29-18-28(35-23-36-29)33-19-24-7-4-3-5-8-24/h3-5,7-10,17-18,23,39,41H,6,11-16,19-22H2,1-2H3,(H,34,40)(H,33,35,36)
• InChIKey: PWYRDVXYAOGDNK-UHFFFAOYSA-N
• SMILES: CC1(CCN(CC1)CC2=CC(=C(C=C2)C(=O)NCC3(CCCN(C3)C4=NC=NC(=C4)NCC5=CC=CC=C5)O)O)C

UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 µM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3[1].
UZH1a (2.5-160 μM; 72 h) inhibits the growth of MOLM-13, HEK293T, and U2Os cells, with IC50s of 11 μM, 67 μM, and 87 μM, respectively[1].
UZH1b (2.5-160 μM; 72 h) inhibits the growth of MOLM-13, HEK293T, and U2Os cells, with IC50s of 78 μM, 79 μM, and 93 μM, respectively[1].
UZH1a (2.5-100 μM; 16 h) reduces m6A methylation level in mRNA from cells in a dose-dependent manner (IC50=4.6 μM), while UZH1b is less active at concentrations up to 100 μM in MOLM-13 cells[1].UZH1a (40 μM; 16 h) reduces m6A methylation level in mRNA from MOLM-13, HEK293T, and U2Os cells[1].
UZH1a (20 μM; 16 h) increases apoptosis and leads to cell cycle arrest in MOLM-13 cells[1].

Reference

[1]. Moroz-Omori EV, et, al. METTL3 inhibitors for epitranscriptomic modulation of cellular processes. bioRxiv. 2020 Oct 13.