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FTO inhibitor Dac51

Chemical Structure : FTO inhibitor Dac51

CAS No.: 2243944-92-3

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FTO inhibitor Dac51 (UUN44923, Dac51)

Catalog No.: PC-38021Not For Human Use, Lab Use Only.

FTO inhibitor Dac51 (Dac51, UUN44923) is a potent, small-molecule compound that can inhibit the activity of m6A demethylase FTO, inhibits FTO-mediated demethylation of m6A with IC50 of 0.4 uM.

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10 mg $128 In stock
25 mg $218 In stock
50 mg $358 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

FTO inhibitor Dac51 (Dac51, UUN44923) is a potent, small-molecule compound that can inhibit the activity of m6A demethylase FTO, inhibits FTO-mediated demethylation of m6A with IC50 of 0.4 uM.
Dac51 is a more potent inhibitor than FB23-2 that binds to and stabilizes FTO, stabilizes the thermal denaturation of the FTO protein in both B16-OVA and LLC cells.
Dac51 treatment B16-OVA and LLC cell lines increased m6A modification on most m6A-marked genes, including Jun and Cebpb.
Dac51 dampened the glycolytic capacity of tumor cells by inhibiting FTO-mediated demethylation on transcripts including Jun and Cebpb; Dac51 increases T cell infiltration and synergizes with anti-PD-L1 blockade in treated B16-OVA cells.
Dac51 treatment (2 mg/kg) effectively inhibited tumor growth in vivo, also significantly increased the proportion of infiltrated CD8+ T cells in the tumor microenvironment, Dac51 delivers strong T cell-mediated antitumor effects and prevents tumor recurrence via memory T cell responses.

Physicochemical Properties

M.Wt 391.25
Formula C18H16Cl2N4O2
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

Benzamide, 2-[[2,6-dichloro-4-(3,5-dimethyl-1H-pyrazol-4-yl)phenyl]amino]-N-hydroxy-

References

1. Yi Liu, et al. Cell Metab. 2021 Jun 1;33(6):1221-1233.e11.

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