Chemical Structure : METTL3 inhibitor UZH2
CAS No.: 2756566-45-5
Catalog No.: PC-49679Not For Human Use, Lab Use Only.
METTL3 inhibitor UZH2 is a potent, selective and cell-permeable RNA methyltransferase METTL3 inhibitor with IC50 of 5 nM in TR-FRET assays.
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METTL3 inhibitor UZH2 is a potent, selective and cell-permeable RNA methyltransferase METTL3 inhibitor with IC50 of 5 nM in TR-FRET assays.
UZH2 displays no affinity against METTL16 and METTL1 in a thermal shift assay at 100 uM.
UZH2 dose-dependently decreased MOLM-13 and PC-3 cell growth following 72 h of incubation, with GI50 values of 12 and 70 μM, respectively.
UZH2 dose-dependently stabilize METTL3, with EC50 values of 2 and 0.85 μM in HEK293T cells and AML MOLM-13 cells through the InCELL Pulse assay and CETSA, respectively.
UZH2 reduced the m6A/A level of polyadenylated RNA in MOLM-13 (acute myeloid leukemia) and PC-3 (prostate cancer) cell lines.
M.Wt | 513.64 | |
Formula | C27H37F2N7O | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
4-(4-((4,4-dimethylpiperidin-1-yl)methyl)-2,5-difluorophenyl)-9-(6-(methylamino)pyrimidin-4-yl)-1,4,9-triazaspiro[5.5]undecan-2-one |
1. Aymeric Dolbois, et al. J Med Chem. 2021 Sep 9;64(17):12738-12760.
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