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METTL3 inhibitor UZH2

Chemical Structure : METTL3 inhibitor UZH2

CAS No.: 2756566-45-5

METTL3 inhibitor UZH2 (UZH2)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 513.64
Formula C27H37F2N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

1. Aymeric Dolbois, et al. J Med Chem. 2021 Sep 9;64(17):12738-12760.

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